The Ninety-Six Most Common Drugs For The Final Control Flashcards

1
Q

What is the MoA for lidocaine? What drug class is it in?

A

Lidocaine cations bind to calcium ions channels, locking them in the open state preventing depolarisation. Prevents transmission and aborts generation. Amide group anaesthetic.

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2
Q

What are the clinical indications for lidocaine?

A

Local or regional anaesthetic by infiltration techniques (percutaneous injection or IV regional anaesthesia by central or peripheral nerve block)

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3
Q

What are the side effects of lidocaine?

A

Nervous agitation, loss of consciousness, respiratory paralysis, decreased BP, bradycardia, cardiac arrest and inhibition of myocardial function.

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4
Q

What are the interactions and contraindications of lidocaine?

A

Cimetedine and propranolol reduce hepatic clearance. Barbiturates, phenytoin and rifampicin reduce effectiveness by induction of microsomal liver enzymes. Sedatives increase CNS inhibition.

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5
Q

What is the MoA for articaine (ultracaine)? What drug class is it in?

A

Hydrolysed articaine binds to and blocks sodium channels preventing depolarisation. Thiophene derivative local anaesthetic.

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6
Q

What are the clinical indications for articaine (ultracaine)?

A

Infiltration and conduction anaesthesia in dentistry.

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7
Q

What are the side effects of articaine (ultracaine)?

A

Loss of consciousness, respiratory depression / paralysis, muscle tremor / twitching –> seizures. Decreases BP, heart failure, shock. Visual disturbances.

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8
Q

What are the interactions and contraindications of articaine (ultracaine)?

A

Enhance action of CNS inhibitors. Anticoagulants increase risk of bleeding. MAOIs increase risk of hypotension. Antagonistic to anti-skeletal drugs (such as those that treat MG). Contraindicated in those with ACG, megaloblastic B12 deficiency anaemia, respiratory conditions and heart conditions such as tachycardia, hypotension and heart failure.

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9
Q

What is the MoA for atropine sulfate? What drug class is it in?

A

Binds to and inhibits muscarinic ACh receptors. Alkaloid (derived from belladonna) anti-muscarinic agent.

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10
Q

What are the clinical indications for atropine sulfate?

A

Treats poisoning by organophosphate nerve agents that have anti-cholinesterase activity (e.g. Neostigmine) Controls symptoms of Parkinson’s disease. Causes mydriasis. Used in ophthalmology to treat inflammatory eye diseases via ciliary muscles relaxation.

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11
Q

What are the side effects of atropine sulfate?

A

Dry mouth, tachycardia, constipation, difficulty urinating, photophobia etc (promotes SNS effects).

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12
Q

What are the interactions and contraindications of atropine sulfate?

A

Atropine absorption decrease when used with antacids. Anticholinergic effect increased when given with other anticholinergic drugs. Increased BP with phenylephrine. Reduced concentration of levodopa.

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13
Q

What is the MoA for pilocarpine hydrochloride? What drug class is it in?

A

Muscarinic agonist. Increases secretion by exocrine glands, causes miosis. Methylimidazole derivative drug.

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14
Q

What are the clinical indications for pilocarpine hydrochloride?

A

Treats radiation induced xerostomia. Treats acute glaucoma, COAG.

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15
Q

What are the side effects of pilocarpine hydrochloride?

A

Headache, follicular conjunctivitis with prolonged use, dermatitis of the eye lid, severe myosis.

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16
Q

What are the interactions and contraindications of pilocarpine hydrochloride?

A

Contraindicated in those with eye diseases where miosis would be undesirable such as iritis. Antagonist of m-anticholinergics such as atropine.

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17
Q

What is the MoA for neostigmine (proserine)? What drug class is it in?

A

Ani-cholinesterase inhibitor. Stimulates nicotinic and muscarinic receptors - therefore improves muscle contraction. Lowers IOP in OAG. Cholinergic group of drugs.

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18
Q

What are the clinical indications for neostigmine (proserine)?

A

Symptomatic treatment of myasthenia gravis (improves muscle tone).

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19
Q

What are the side effects of neostigmine (proserine)?

A

GI symptoms, miosis, loss of consciousness, headache, arrhythmias, AV block, decreased BP, SOB, respiratory depression.

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20
Q

What are the interactions and contraindications of neostigmine (proserine)?

A

Contraindicated in epilepsy, CVD, CAD, heart disease in general, GI obstruction. Enhances action of depolarising muscle relaxants, and antagonist of non-depolarising muscle relaxants. Effect reduced when used with m-anticholinergics, ganglionic blockers, antidepressants etc. Ephedrine increases the effect.

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21
Q

What is the MoA for suxamethonium chloride (succinylcholine / dithylin)? What drug class is it in?

A

Persistent depolarisation of NMJ as dithylin mimicks ACh but is not rapidly hydrolysed by acetylcholinesterase. Depolarising neuromuscular blocker.

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22
Q

What are the clinical indications for suxamethonium chloride (succinylcholine / dithylin)?

A

Used in surgical procedures where rapid but brief muscle relaxation is required - such as in intubation, endoscopies and ECT.

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23
Q

What are the side effects of suxamethonium chloride (succinylcholine / dithylin)?

A

Hyperkalaemia, decreased BP, arrhythmia, bradycardia, respiratory paralysis, increased IOP.

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24
Q

What are the interactions and contraindications of suxamethonium chloride (succinylcholine / dithylin)?

A

ACG, MG, Duchennes, pulmonary oedema, hyperkalaemia. Anticholinesterase inhibitors, bradycardia, decreases effectiveness of MG drugs.

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25
What is the MoA for epinephrine? What drug class is it in?
Adrenergic agonist. Strongest alpha receptor agonist. Causes vasoconstriction, relaxes smooth muscle (beta-2-receptors), increased heart rate and cardiac output (beta-1-receptor) histamine antagonist, increases blood sugar levels (glycogenolysis in the liver).
26
What are the clinical indications for epinephrine?
Emergency treatment of type I allergic reactions. Restores cardiac rhythm in cardiac arrest. Maintains mydriasis. Treats symptoms of asthma.
27
What are the side effects of epinephrine?
Angina pectoris, reflex bradycardia / tachycardia, reflex hypotension, anxiety, headache, fatigue, nausea, vomiting, prostatic hyperplasia, hypokalaemia, hyperglycemia
28
What are the interactions and contraindications of epinephrine?
Contraindicated in hypertrophic obstructive cardiomyopathy, pheochromocytoma, pregnancy, lactation.
29
What is the MoA for phenylephrine (mesatone)? What drug class is it in?
Alpha 1 adrenergic agonist. Causes vasoconstriction, mydriasis, raises BP by increasing peripheral resistance and stimulating the vagus nerve (reflex bradycardia).
30
What are the clinical indications for phenylephrine (mesatone)?
Injection treats hypotension. Ophthalmic preparation dilates pupils. Treats congestion. Topically treats haemorrhoids.
31
What are the side effects of phenylephrine (mesatone)?
Increases BP long term, tachycardia / reflex bradycardia.
32
What are the interactions and contraindications of phenylephrine (mesatone)?
Those with arterial hypertension, severe atherosclerosis, spasm of coronary vessels. When used in conjunction with general anaesthesia may cause ventricular fibrillation. MAOIs increase effect. Oxytocin and TCAs enhance pressor effect.
33
What is the MoA for propranolol (anaprilin)? What drug class is it in?
Non-selective beta adrenergic antagonist. Causes vasoconstriction, inhibits angiogenic factors (VEGF, bFGF), induces endothelial cell apoptosis, down regulates RAAS. Reduces AV conduction, therefore reduces HR.
34
What are the clinical indications for propranolol (anaprilin)?
Treats hypertension, angina pectoris, AF, MI, essential tremor, migraine, pheochromocytoma.
35
What are the side effects of propranolol (anaprilin)?
Dry sore eyes, bradycardia, AV block, GI symptoms, congestion, bronchospasm, changes in blood glucose concentration, haemopoetic changes.
36
What are the interactions and contraindications of propranolol (anaprilin)?
Contraindicated in those with AV / SA block, CVD, MI, pheochromocytoma, MAOIs, hypoglycaemic events and inhaled anaesthetics.
37
What is the MoA for metoprolol? What drug class is it in?
Beta-1 antagonist (specific to cardiac cells) negligible effect on beta-2. Decreases cardiac output by suppressing calcium release. Decreases slope of phase 4 and prolong repolarization of phase 3.
38
What are the clinical indications for metoprolol?
Treats angina, heart failure, MI, AF, atrial flutter and hypertension.
39
What are the side effects of metoprolol?
Sinus bradycardia, decreased BP, orthosttic hypotension, chronic heart failure, arrhythmia, mental disturbances, seizures, nasal congestion, bronchospasm (high doses), GI disturbances.
40
What are the interactions and contraindications of metoprolol?
Contraindicated in II and III degree AV block, heart failure, those taking drugs affecting beta receptors (long term), bradycardia, hypotension, severe COPD, pheochromocytoma, MAOIs and calcium channel blockers. Therefore, should not be used concurrently with antihypertensives, diuretcs, antiarrhythmic drugs, hypoglycaemic agents, NSAIDs, opioids, peripheral muscle relaxants, contraceptives, cimetedine and amiodarone.
41
What is the MoA for dobutamine? What drug class is it in?
Beta-1 agonist that increases contractility and cardiac output (positive inotropic effect). Increases cAMP and calcium release.
42
What are the clinical indications for dobutamine?
Parenteral therapy for inotropic support in (short term) treatment of patients with cardiac decompensation due to depressed contractility resulting either from organic heart disease or from cardiac surgical procedures.
43
What are the side effects of dobutamine?
Eosinophilia, tachycardia, hypertension, arrhythmias, vasoconstriction, MI, ST segment elevation, urge to urinate.
44
What are the interactions and contraindications of dobutamine?
Contraindicated in those with ventricular arrhythmias, pheochromocytoma, mechanical obstruction to blood flow, lactation. Interactions with MAOIs, beta-blockers, cardiac glycosides, dipyridamole, dopamine, nitroglycerin, ACE inhibitors, COMT inhibitors, inhaled anaesthetics, TCAs, levodopa and thyroid hormones.
45
What is the MoA for salbutamol (albuterol)? What drug class is it in?
Short acting beta-2 agonist. Beta-2 receptors found on airway smooth muscle. Activates adenylate cyclase, increasing cAMP preventing PKA from phosphorylating myosin. Also lowers intracellular calcium. Increased cAMP also inhibits release of inflammatory mediators from mast cells.
46
What are the clinical indications for salbutamol (albuterol)?
Used for symptomatic relief and prevention of bronchospasm in bronchial asthma, chronic bronchitis, reversible obstructive airway disease and in prophylaxis of exercise induced bronchospasm.
47
What are the side effects of salbutamol (albuterol)?
Expansion of peripheral vessels, tachycardia, hypokalaemia and tremors.
48
What are the interactions and contraindications of salbutamol (albuterol)?
Contraindicated in children under two years of age. Suppression of therapeutic effect when used with non-cardio selective beta blockers. Theophylline increases risk of cardiac effects. Xanthine derivates, corticosteroids and diuretics increase the risk of hypokalaemia.
49
What is the MoA for reserpine? What drug class is it in?
Inhibits ATP/Mg2+ pump preventing the release of NTs, the NTs in the vesicles are degraded by MAOIs.
50
What are the clinical indications for reserpine?
Treats hypertension.
51
What are the side effects of reserpine?
Bradycardia, increases symptoms of angina pectoris, urinary retention, weight gain, decreased libido.
52
What are the interactions and contraindications of reserpine?
Contraindicated in those with ulcers in the exacerbation phase, bronchial asthma, bradycardia. Increases the effects of direct acting-sympathomimetics. Bradycardia when used with digoxin. Enhancement of barbiturate effects.
53
What is the MoA for chlorpromazine (aminazine)? What drug class is it in?
Dopamine, 5-HT, H, alpha, muscarinic receptor antagonist. Presynaptic inhibitor of dopamine re-uptake.
54
What are the clinical indications for chlorpromazine (aminazine)?
Treatment of schizophrenia (controls nausea and vomiting), controls manic-depressive illnesses, control of severe behavioural problems in children.
55
What are the side effects of chlorpromazine (aminazine)?
Akathisia, vision impairment, dystonic extrapyrimidal effects (parkinsonism syndrome), tardive dyskinesia, hypotension, tachycardia, dypepsia, menstrual irregularities, impotence, gynecomastia, weight gain.
56
What are the interactions and contraindications of chlorpromazine (aminazine)?
Contraindicated in patients with hepatic, blood forming organ or renal dysfunction, myxedema (hypothyroidism), diseases of the CNS, cardiovascular disease, ACG, urinary retention and prostatic hyperplasia. Major interactions with clozapine, haloperidol and escitalopram.
57
What is the MoA for droperidol? What drug class is it in?
Antidopaminergic action and weak anticholinergic action. Antagonises glutamic acid within the extrapyramidal system. Acts on mesolimbic and mesocortical pathways in the brain.
58
What are the clinical indications for droperidol?
Used as an antiemetic (such as in surgical and diagnostic procedures). Acts on the chemoreceptor trigger zone.
59
What are the side effects of droperidol?
Dysphoria, drowsiness (post-operatively), hypotension and tachycardia, nausea, vomiting, loss of appetite.
60
What are the interactions and contraindications of droperidol?
Contraindicated in those with extra-pyrimidal disorders (such as Parkinson's disease), depression, hypokalaemia, hypotension, increased QT intervals. When droperidol is used simultaneously with CNS depressants the CNS inhibition is enhanced. Antagonises epinephrine and sympathomimetic agents. Potentiates the action of antihypertensives. Inhibits action fo dopamine agonists.
61
What is the MoA for diazepam (sibazon)? What drug class is it in?
Benzodiazepine tranquiliser (anticonvulsant, sedative, muscle relaxant). Binding increases inhibitory effect of GABA (GABA agonist).
62
What are the clinical indications for diazepam (sibazon)?
Symptomatic management of anxiety. Symptomatic relief in alcohol withdrawal. Relieves skeletal muscle spasm. Cerebral palsy. Myoclonus epilepsy.
63
What are the side effects of diazepam (sibazon)?
Drowsiness, fatigue, impaired attention, ataxia, slowed mental and motor reactions, anterograde amnesia, decreased appetite, nausea, vomiting (GI disturbances), tachycardia, hypotension.
64
What are the interactions and contraindications of diazepam (sibazon)?
Contraindicated in patients with hepatic impairment, ACG, with alcohol, CNS depressants. Interacts with codeine, hydrocodone, oxycodone and tramadol.
65
What is the MoA for nitrazepam? What drug class is it in?
Benzodiazepine tranquiliser (anticonvulsant, sedative, muscle relaxant). Binding increases inhibitory effect of GABA (GABA agonist).
66
What are the clinical indications for nitrazepam?
Treats short term insomnia.
67
What are the side effects of nitrazepam?
Fatigue, cognitive impairment, muscle weakness, change in libido.
68
What are the interactions and contraindications of nitrazepam?
Contraindicated in patients with acute respiratory failure, alcohol dependence, MG, temporal lobe epilepsy, ACG. Interacts with anaesthetics and anticonvulsants such as carbamazepine and phenytoin.
69
What is the MoA for sodium valproate? What drug class is it in?
Sodium channel blockade, blockade of GABA transaminase, T-type calcium channel blocker.
70
What are the clinical indications for sodium valproate?
Treats focal and primary generalised epilepsy.
71
What are the side effects of sodium valproate?
Trembling of hand(s), mild cramping in the abdomen and stomach, loss of appetite, GI disturbances,, thrombocytopenia, menstrual irregularities.
72
What are the interactions and contraindications of sodium valproate?
Contraindicated in patients with severe liver dysfunction, pancreatic dysfunction, porphyria, who are pregnant or breast feeding. Interacts with anti-depressants such as amitriptyline, other anti-epileptics such as ethosuximide and phenytoin, rifampicin and warfarin.
73
What is the MoA for phenobarbital? What drug class is it in?
GABA-A agonist. Elevates seizure threshold (reducing spread of seizure from focus). Calcium channel blocker decreasing excitatory transmitter release. Sedative hypnotic effect as acts in midbrain reticular formation controlling arousal.
74
What are the clinical indications for phenobarbital?
Treats seizures (sans absence seizures).
75
What are the side effects of phenobarbital?
Weakness, drowsiness, fatigue, ataxia, depression.
76
What are the interactions and contraindications of phenobarbital?
Contraindicated in those with severe hepatic and renal insufficiency or porphyria. Interacts with warfarin, HRT, MAOIs, antidepressants, other anti-epileptics, sedatives, tranquillisers.
77
What is the MoA for levodopa / carbidopa? What drug class is it in?
Crosses the BBB and is decarboxylated to form dopamine. Given with carbidopa (dopamine decarboxylase inhibitor) to prevent peripheral conversion.
78
What are the clinical indications for levodopa / carbidopa?
Treats Parkinson's disease. Decreases rigidity, tremors. Effectiveness is reduced after 3 - 5 years. Withdrawal must be gradual.
79
What are the side effects of levodopa / carbidopa?
Anorexia, nausea, vomiting (stimulates chemoreceptor trigger zone), tachycardia, and ventricular extrasystole (due to dopamines effect on the heart), hypotension, mydriasis, brown urine due to products of catecholamine oxidation. Visual / auditory hallucinations, dyskinesia, mood changes, depression, anxiety, psychosis.
80
What are the interactions and contraindications of levodopa / carbidopa?
Interacts with pyridoxine as it causes peripheral degradation of levodopa. MAOIs in conjunction with levodopa can cause a hypertensive crisis. Exacerbates symptoms in psychotic patients (such as schizophrenics). Antipsychotic drugs are contraindicated due to their antagonistic affect to levodopa.
81
What is the MoA for ketamine? What drug class is it in?
NMDA antagonist. Short acting non-barbiturate anaesthetic. Dissociative anaesthesia providing sedation, amnesia and immobility. Stimulates central sympathetic outflow increasing cardiac output and blood pressure. Also used as a bronchodilator.
82
What are the clinical indications for ketamine?
Used as an (induction) anaesthetic in short procedures. Also used to treat hypovolemic and cardiogenic shock as well as in asthmatics. Possible management of depression at low doses.
83
What are the side effects of ketamine?
Increases cerebral blood flow and may induce hallucinations (potential drug of abuse). Muscle stiffness, oppression of respiratory centre, diplopia, nystagmus, increased IOP, SOB, obstruction of RT, increased BP, hypersalivation.
84
What are the interactions and contraindications of ketamine?
Contraindicated in hypertensive and stroke patients. Enhances action fo CNS depressants. Enhances muscle relaxant activity.
85
What is the MoA for ethyl alcohol? What drug class is it in?
GABA agonist.
86
What are the clinical indications for ethyl alcohol?
Methanol intoxification
87
What are the side effects of ethyl alcohol?
Intoxification, low BP, agitation, low blood sugar, nausea, vomiting, excessive urination
88
What are the interactions and contraindications of ethyl alcohol?
Brain operations, coma, diabetes, alcoholism, low BP, liver/renal probelms,
89
What is the MoA for morphine hydrochloride? What drug class is it in?
Acts on kappa receptors in lamina fo the dorsal horn of the spinal cord decreasing substance P release. Mu and kappa opioid receptor agonist in ventral tegmental area of the brain. Also binds to delta receptors in nucleus accumbens (reward pathway). Mu receptors (modification of respiratory system and addiction).
90
What are the clinical indications for morphine hydrochloride?
Management of chronic severe pain. Depresses cough reflex.
91
What are the side effects of morphine hydrochloride?
Respiratory depression, dependence, addiction, tolerance, severe withdrawal symptoms, nausea, urinary retention, constipation, sedation, hypotension, dysphoria.
92
What are the interactions and contraindications of morphine hydrochloride?
Contraindicated in patients with asthma, liver disease and renal dysfunction. Interacts with phenothiazines, MAOIs and TCAs. Naloxone and nalorphine reverse the effects of opioid agonists.
93
What is the MoA for trimeperidine (promedol)? What drug class is it in?
Opioid receptor agonist. Lesser effect on the respiratory system than morphine. Produced analgesia by kappa receptor mediated reduction in substance P release.
94
What are the clinical indications for trimeperidine (promedol)?
Management of chronic severe pain. Depresses cough reflex.
95
What are the side effects of trimeperidine (promedol)?
Nausea, vomiting, weakness, dizziness, euphoria, disorientation.
96
What are the interactions and contraindications of trimeperidine (promedol)?
Contraindicated in those with respiratory depression. Enhancement of drugs that suppress the CNS. Analgesic effect is reduced when used with barbiturates such as phenobarbital. Naloxone and nalorphine reverse the effects of opioid agonists.
97
What is the MoA for fentanyl? What drug class is it in?
Binds to mu opioid receptors. Down regulates adenylate cyclase, reduces cAMP and cAMP dependant influx of calcium into the cell. Exchange of GTP and GDP leads to hyperpolarisation.
98
What are the clinical indications for fentanyl?
Short term analgesia and anaesthesia (induction and maintenance). Control of chronic pain.
99
What are the side effects of fentanyl?
Drowsiness, confusion, hallucinations, euphoria, muscle stiffness, bradycardia, nausea, vomiting, constipation, respiratory depression, urinary retention.
100
What are the interactions and contraindications of fentanyl?
Contraindicated in those with asthma, drug addiction, conditions involving respiratory depression, obstetric surgery. Enhancement of drugs that suppress the CNS. Analgesic effect is reduced when used with barbiturates such as phenobarbital. Naloxone and nalorphine reverse the effects of opioid agonists.
101
What is the MoA for naloxone? What drug class is it in?
Competitive antagonist of opioid receptors (binds strongly to mu, but does bind to all three).
102
What are the clinical indications for naloxone?
Reversal of narcotic (respiratory) depression induced by opioids.
103
What are the side effects of naloxone?
Tachycardia, hypo/hypertension, ventricular fib, pulmonary oedema, nausea, vomiting, trembling, increased sweating.
104
What are the interactions and contraindications of naloxone?
Contraindicated in those with hypersensitivity to naloxone. Naloxone may decrease the antihypertensive effect of clonidine.
105
What is the MoA for acetylsalicylic acid (aspirin)? What drug class is it in?
Inhibits thromboxane A2 synthesis by acetylation of serine residue on active site of COX-1. irreversibly inactivating the enzyme. Shifts balance of chemical mediators to favour antiaggregatory effects of prostacyclin preventing platelet aggregation.
106
What are the clinical indications for acetylsalicylic acid (aspirin)?
Prophylactic treatment of transient cerebral ischaemia, reduces incidence of recurrent MI, complete inactivation of platelets when 75mg is taken daily.
107
What are the side effects of acetylsalicylic acid (aspirin)?
Angioedema, bleeding, bronchospasm, GI disturbances, reye syndrome in under 16s and Stevens - Johnson syndrome.
108
What are the interactions and contraindications of acetylsalicylic acid (aspirin)?
Interacts with keterolac (increases bleeding), cidofovir (nephrotoxicity), probenecid (decreased uricosuric effects). Contraindicated in patients who are at risk of increased bleeding.
109
What is the MoA for diclofenac sodium? What drug class is it in?
Phenylacetic acid derivative, NSAID, COX-1 / 2 (preferably COX-2) inhibitor. Reduces production of PGs which in turn reduces pain, swelling (inflammation in general).
110
What are the clinical indications for diclofenac sodium?
Treatment of pain and inflammation and pain in osteoarthritis, rheumatoid arthritis, akylosing spondylitis.
111
What are the side effects of diclofenac sodium?
Erythema, dermatitis, hypertension, nasal congestion, diarrhoea, constipation.
112
What are the interactions and contraindications of diclofenac sodium?
Attack of bronchial asthma, urticaria, acute rhinitis when taking other NSAIDs. Reduced skin integrity when applied topically. Contraindicated in pregnant women and lactation. Interacts with photosensitising medications.
113
What is the MoA for paracetamol? What drug class is it in?
Inhibits PG synthesis (antipyretic and analgesic). Lesser effect on COX in the periphery (weak anti-inflammatory effect). Does not affect platelet function.
114
What are the clinical indications for paracetamol?
Alternative analgesic for those who complain of gastric complaints or have prolonged bleeding time and those who do not require anti-inflammatory action of NSAIDs. Also antipyretic - preferred drug for children with viral infections (including chicken pox).
115
What are the side effects of paracetamol?
Large doses deplete glutathione in liver. May cause hepatic necrosis.
116
What are the interactions and contraindications of paracetamol?
Should be avoided in patients with hepatic impairment. Abuse of alcohol increases risk of paracetamol induced hepatotoxicity.
117
What is the MoA for celecoxib? What drug class is it in?
NSAID. Selective COX-2 inhibitor (reversible) reducing production of PGE2.
118
What are the clinical indications for celecoxib?
Treats rheumatoid arthritis, osteoarthritis, acute to moderate pain.
119
What are the side effects of celecoxib?
Headache, dyspepsia, diarrhoea, abdominal pain.
120
What are the interactions and contraindications of celecoxib?
Contraindicated in in patients who are taking aspirin for CV prevention and who are at high risk of ulcers. Fluconazole increases serum levels of celecoxib.
121
What is the MoA for meloxicam? What drug class is it in?
NSAID, oxicam, COX- 1, 2 inhibitor (COX-2 preferential binding). Inhibits PG synthesis. Analgesic and inflammatory effects.
122
What are the clinical indications for meloxicam?
Symptomatic relief in arthritis, osteoarthritis, juvenile rheumatoid arthritis.
123
What are the side effects of meloxicam?
GI disturbances, hypertension, triggers cytopenia, gastrointestinal bleeding.
124
What are the interactions and contraindications of meloxicam?
Contraindicated in patients with hepatic and renal insufficiency, those with bronchial asthma, hypertension, CVD. Interacts with ACE inhibitors, angiotensin II receptor blockers, diuretics. May increase the risk of bleeding so should not be taken with anticoagulants and anti-platelet drugs.
125
What is the MoA for caffeine sodium benzoate? What drug class is it in?
Adenosine receptor antagonist.
126
What are the clinical indications for caffeine sodium benzoate?
Stimulates CNS, heightening alertness, causing restlessness, relaxes smooth muscle, contract cardiac muscle, promotes gastric secretion, relieves symptoms of migraine. Mild diuretic.
127
What are the side effects of caffeine sodium benzoate?
Agitation, anxiety, tremor, headache, tachypnea, tinnitus, insomnia, tachycardia, arrhythmias, hypertension, nausea, vomiting, nasal congestion.
128
What are the interactions and contraindications of caffeine sodium benzoate?
Contraindicated in those with anxiety disorders, hypertension, glaucoma and epilepsy. Stimulants should be avoided.
129
What is the MoA for piracetam? What drug class is it in?
Nootropic. Increases glucose utilisation and improves microcirculation in ischaemic zones. Therefore, has a protective effect in cases of brain damage. Interacts with polar heads of PLs reducing curvature caused by amyloid peptides.
130
What are the clinical indications for piracetam?
Used in cases of memory impairment such as dementia due to CVA or Alzheimer's. Treats myoclonus of cortical origin but should be used in combination with anti-myoclonic therapies.
131
What are the side effects of piracetam?
Increased sexual activity, dyspeptic symptoms, abdominal pain, nervousness, agitation, anxiety, irritability.
132
What are the interactions and contraindications of piracetam?
Contraindicated in hemorrhagic stroke, severe renal failure. When used in combination with thyroid hormones can cause tremor, anxiety, irritability and confusion. With CNS stimulants enhances psycho-stimulating effect. When used with antipsychotics increases extrapyramidal effects.
133
What is the MoA for amitriptyline? What drug class is it in?
Tricyclic antidepressant. Inhibits NT reuptake into presynaptic nerve terminals. Blocks serotonergic, alpha adrenergic, histaminic and muscarinic receptors. They elevate mood, improve alertness, increase activity, reduce morbid preoccupation. Onset is slow (~ 2 weeks).
134
What are the clinical indications for amitriptyline?
Treat moderate to severe depression. Also prevents migraine and headache and treats chronic pain syndromes (neuropathic) can also treat insomnia.
135
What are the side effects of amitriptyline?
Muscarinic blocking = blurred vision, xerostomia, urinary retention, tachycardia, constipation, ACG aggravation. Blockage of alpha receptors = hypotension and reflex tachycardia. H1 = sedation. Sexual dysfunction and weight gain.
136
What are the interactions and contraindications of amitriptyline?
Contraindicated in patietns with bipolar disorder, even in depressed state as may cause a switch to manic behaviour. Risk of suicide. Exacerbate BPH, epilepsy and arrhythmias. Toxic sedation occurs with ethanol and other CNS depressants. MAOIs lead to mutual enahncement, hypertension, hyperpyrexia, convulsions and coma, direct acting adrenergic drugs potentiate the effects of biogenic amine drugs by preventing removal from synaptic cleft. Indirect acting adrenergic drugs prevents drugs from reaching their cellular sites of action.
137
What is the MoA for fluoxetine? What drug class is it in?
SSRIs - selectively inhibit serotonin re-uptake increasing 5-HT in the synaptic cleft.
138
What are the clinical indications for fluoxetine?
Treat depression. Also indicated for OCD, panic disorders, generalised anxiety, PTSD, social anxiety, premenstrual dysphoric disorder and bulimia nervosa.
139
What are the side effects of fluoxetine?
Headache, sweating, anxiety, agitation, GI effects, weakness, sexual dysfunction, weight gain, sleep disturbance, hyponatremia.
140
What are the interactions and contraindications of fluoxetine?
Interacts with anti-platelet drugs, NSAIDs and MAOIs. Contraindicated in those more at risk of bleeding, those with manic behaviour, suicidal thoughts, diabetes and excess antidiuretic hormone.
141
What is the MoA for L-thyroxine? What drug class is it in?
Synthetic version and isomer of T4. This supresses production of TSH from the anterior pituitary gland. In the periphery it is converted to T3. This increases metabolic rate, maintains brain function and is involved in food metabolism, maintains temperature. It does this by binding to TRE gene. This regulates heart rate, cardiac output and systemic vascular resistance. T4 binds to integrin aVb3 activating mitogen-activated protein kinases leading to angiogenesis and tumour cell proliferation. Hormone class of drugs.
142
What are the clinical indications for L-thyroxine?
Used as replacement therapy in primary, secondary and tertiary hypothyroidism. It is also indicated in the management of thyrotropin-dependent well differentiated thyroid cancer.
143
What are the side effects of L-thyroxine?
L-thyroxine increases appetite, can also cause weight loss, heat sensitivity, excessive sweating, headache, hyperactivity, nervousness, anxiety, irritability, mood swings, trouble sleeping, tiredness, tremors, muscle weakness, changes in menstrual periods, hair loss, diarrhoea, vomiting and stomach cramps. Can also cause heart attacks, heart failure, tachycardia and irregular heart rhythm.
144
What are the interactions and contraindications of L-thyroxine?
The risk of side effects are increased when combined with antidepressant, sympathomimetics, blood thinners and ketamine. Antiepileptics, CaCO3, FeSO4, cancer drugs and tyrosine kinase inhibitors reduce the effectiveness of L-Thyroxine.
145
What is the MoA for insulin? What drug class is it in?
Produced by the beta cells in the islets of langerhan. Promotes glucose metabolism and storage. Inhibits production of glucose and increases DNA production. Binds to alpha subunits of insulin receptor and leads to tyrosine kinase activity in the beta subunits. Downstream signalling of Akt regulating GLUT4 transporters as well as PKC activity. Insulin class of drugs.
146
What are the clinical indications for insulin?
Used in the treatment of hyperglycaemia associated with type I and II DM. Primarily in type I due to destruction of beta cells and the complete lack of endogenous insulin. Also useful when there is cellular resistance to insulin due to high blood glucose concentration.
147
What are the side effects of insulin?
Swelling of arms and legs, weight gain, hypoglycaemia (which includes sweating, shaking, hunger, tachycardia, neuropathy, confusion, blurred vision, slurred speech and anxiety), injection site reaction, lipodystrophy, hypokalaemia and heart failure.
148
What are the interactions and contraindications of insulin?
Interactions based on other drugs affecting blood glucose concentration requiring dose alterations. This occurs with thiazolidinediones, MAOIs, antidiuretics, corticosteroids, oestrogen, isoniazid, HIV drugs, sulphonamides and thyroxine.
149
What is the MoA for glibenclamide? What drug class is it in?
Closes ATP-sensitive K+ channels on pancreatic beta cells (sulfonylurea receptor 1). At low glucose concentration the channel is open, the K+ efflux creates a -70mV membrane potential. At high concentrations it closes depolarising the cell, opening gated calcium channels releasing insulin from granules. Glibenclamide forces these channels closed leading to insulin release. Sulfonylurea drug class.
150
What are the clinical indications for glibenclamide?
Indicated as single line or combination treatment with metformin to improve control of blood glucose concentration in type II DM.
151
What are the side effects of glibenclamide?
Nausea, vomiting, constipation, diarrhoea, hypoglycaemia and weight gain.
152
What are the interactions and contraindications of glibenclamide?
Contraindicated in those: experiencing ketoacidosis, infection, undergoing surgery, experiencing trauma and TI DM, thyroid diseases, children and pregnant women. Should not be taken by those with hepatic or renal impairment or with G6PD deficient (haemolytic amaemia).
153
What is the MoA for prednisolone? What drug class is it in?
Corticosteroid - decreases vasodilation and permeability of capillaries. Decreases leukocyte migration to sites of inflammation. Binds to glucocorticoid receptors controlling gene expression - long term effect. Inhibits: neutrophil apoptosis, demargination, PLA2 (decreasing formation of arachidonic acid), NF Kappa B and other inflammatory transcription factors while promoting anti-inflammatory genes like IL-10.
154
What are the clinical indications for prednisolone?
Indicated in the treatment of endocrine, rheumatic, and hematologic disorders. Also used in the treatment of collagen, dermatologic, ophthalmic, respiratory and GI diseases. Can be used to treat allergic and oedematous states as well as tuberculous meningitis.
155
What are the side effects of prednisolone?
Common side effects include acne, dry skin, bruising, nausea, bloating, sweating, slow wound healing, headache, increased appetite, weight gain, mild dizziness, menstrual period changes. More seriously can cause vision problems, swelling or rapid weight gain, shortness of breath, seizures, depression, chest pain, haemoptysis, signs of pancreatitis, signs of low potassium, high BP and severe allergic reaction.
156
What are the interactions and contraindications of prednisolone?
Interacts with aspirin, diuretics, blood thinners, cyclosporine, chemotherapy, insulin, ketoconazole, rifampin, phenobarbital, oral contraceptives and St. John’s Wort.
157
What is the MoA for oxytocin? What drug class is it in?
Produced in the hypothalamus and stored in the posterior pituitary gland. Release is triggered by high plasma osmolality or parturition. Binds to receptors on the uterine myometrium triggering GPCR transduction leading to intracellular calcium release. Activated myosin light chain kinase phosphorylating the myosin light chain, forming actomyosin and triggering smooth muscle contraction. This also occurs in the mammary glands.
158
What are the clinical indications for oxytocin?
Used in obstetrics to stimulate uterine contractions and induce labour. Also stimulates ejection of milk by causing contraction of myoepithelial cells around mammary alveoli.
159
What are the side effects of oxytocin?
May cause hypertension, uterine rupture, water retention and foetal death.
160
What are the interactions and contraindications of oxytocin?
Not to be given to patients during labour and those experiencing an obstruction during delivery. Can also cause foetal death if given in the first 3 trimesters of pregnancy. When given with inhalation anaesthetics increases hypotensive effect and decreases stimulating effect on uterus. PGs increase the effect.
161
What is the MoA for retinol acetate? What drug class is it in?
Oxidised to retinoic acid (vitamin A derivative). Translocates to nucleus binding to intra-nuclear receptor binding to chromatin activating gene transcription.
162
What are the clinical indications for retinol acetate?
Treats acne, psoriasis, photoaging and other skin conditions. Stimulates immune response at cellular and humoral levels. Plays a role in metabolic function of the retina, the growth of epithelial tissue and bone as well as reproduction and the immune response.
163
What are the side effects of retinol acetate?
High levels can leads to irritation and skin pealing / dryness. Can cause photosensitivity as well as dry eyes and mucous membranes.
164
What are the interactions and contraindications of retinol acetate?
It is contraindicated in pregnancy as can cause birth defects (more associated with isotretinoin itself). Should not be taken in conjunction with neomycin, warfarin, orlistat and mineral oil.
165
What is the MoA for pyridoxine hydrochloride? What drug class is it in?
Vitamin B6 (water soluble). PH converted into pyridoxal 5-phosphate. It is a coenzyme for synthesis of AAs, NAs, NTs, SLs,
166
What are the clinical indications for pyridoxine hydrochloride?
Treats B6 deficiency and as prophylaxis for isoniazid induced peripheral neuropathy (as isoniazid inhibits the action of pyridoxine). Used in combination with doxylamine to treat nausea and vomiting in pregnancy.
167
What are the side effects of pyridoxine hydrochloride?
May cause hyper-secretion of HCl.
168
What are the interactions and contraindications of pyridoxine hydrochloride?
Potentiates the effects of diuretics, reduces the effects of levodopa, decreases plasma concentration of phenytoin and phenobarbital, oral contraceptives decrease the effectiveness of pyridoxine hydrochloride.
169
What is the MoA for ascorbic acid? What drug class is it in?
Increases the production of proline and therefore collagen. Important for formation of connective tissue / vessel walls. It is a cofactor in the formation fo 4 – hydroxproline. Also involved in tyrosine metabolism, the conversion of folic acid, carbohydrate metabolism, synthesis of lipids and proteins, iron metabolism and resistance to infections and cellular respiration. Water soluble vitamin (C).
170
What are the clinical indications for ascorbic acid?
It is used in the treatment of vitamin C deficiency, scurvy, delayed wound and bone healing, urine acidification, and as a general antioxidant.
171
What are the side effects of ascorbic acid?
In high doses causes diarrhoea, dizziness, flushing, headache, increased micturition, nausea and vomiting and stomach cramps.
172
What are the interactions and contraindications of ascorbic acid?
Mildly contraindicated in patients with haemolysis, with kidney stones and on dialysis.
173
What is the MoA for tocopherol acetate? What drug class is it in?
An antioxidant the modifies PKC inhibiting cell death. It therefore, has AI effects due to modulation of cytokines, PGs, prostanoids and TXs as the COX pathway is not fed by arachidonic acid. It is also a radical scavenger; an antioxidant for the lipid bilayer. It does this by being a proton donor to alkyls and peroxyls. Fat soluble vitamin (E).
174
What are the clinical indications for tocopherol acetate?
Treats vitamin E deficiency (such as in low weight premies). As it is fat soluble may be required in those with fat malabsorption of patients with abetalipoproteinemia.
175
What are the side effects of tocopherol acetate?
At high doses may cause haemorrhagic activity.
176
What are the interactions and contraindications of tocopherol acetate?
Interactions are related to drugs that reduce or increase the excretion of tocopherol. High amounts of tocopherol lead to interactions with aspirin, warfarin, tamoxifen and cyclosporine A.
177
What is the MoA for cyanocobalamin? What drug class is it in?
Cofactor for methionine (made from homocysteine - also requires B12) synthase (synthesis of purines and pyrimidines) and L-methylmalonyl-CoA mutase (converts L-methylalonyl-CoA to succinyl-CoA [required for Hb synthesis] in the degradation of propionate). This reaction is required for fat and protein metabolism. Tetrahydrofolate required B12 to be regenerated from 5-methyltetrahydrofolate; this leads to folate deficiencies. B12 incorporated folic acid into RBCs - a lack of B12 leads to megaloblastic anaemia.
178
What are the clinical indications for cyanocobalamin?
Used in the treatment of B12 deficiency. Mainly to treat the neurological manifestations. B12 deficiency is due to malabsorption in the following conditions (addisonian anaemia, GI pathologies, fish tapeworm, pancreatic and bowel malignancies, folic adic deficiency). Can also be caused by pregnancy, thyrotoxicosis, hemolytic anaemia, hepatic and renal disease, haemorrhage.
179
What are the side effects of cyanocobalamin?
Injection site pain, arthralgia, dizziness, headache, nasopharyngitis, anaphylaxis.
180
What are the interactions and contraindications of cyanocobalamin?
Contraindicated in patients with thromboembolism, erythremia and erythrocytosis. Interacts with PPIs (may decrease oral absorption of vitamin B12). Colchicine, metformin, antibiotics (gentamycin), antiepileptics and drugs for heart burn reduce absorption of B12.
181
What is the MoA for heparin? What drug class is it in?
Binds to anti-thrombin III increasing the speed at which ATIII inactivates thrombin IIa and factor Xa. The complex also inactivated factors IX, XI, XII and plasmin. N.B it does not have thrombolytic or fibrinolytic action merely prevents further clotting. Anticoagulant drug.
182
What are the clinical indications for heparin?
prophylactic treatment of venous thrombosis and post-operative DVT and PE. Also prevents clotting in arterial and cardiac surgeries. Prevents embolism in patients with AF. Prevents clotting during dialysis. Maintains the patency of IV devices and prevents coagulation of blood transfusions. It is also used in combination with platelet glycoprotein IIb / IIIa receptor inhibitors for unstable angina and non-Q wave MIs. Affects reversed by protamine sulfate.
183
What are the side effects of heparin?
Thrombocytopenia (delayed reaction), mild pain, hematoma, haemorrhage, local irritation, increased liver aminotransferase, osteoporosis.
184
What are the interactions and contraindications of heparin?
Severe interaction include corticorelin, defibrotide mifepristone and prothrombin. Contraindicated in patients with uncontrolled active bleeding and in situations when a coagulation test cannot be performed.
185
What is the MoA for warfarin? What drug class is it in?
Vitamin K antagonist. Disrupts gamma - carboxylation of VII, IX, X, thrombin, protein C and S by binding to vit K epoxide reductase complex subunit 1. Anticoagulant drug.
186
What are the clinical indications for warfarin?
Prophylaxis and treatment of DVT and PE (associated with AF, cardiac valve replacement) Reduces potential for recurring (and reduces the risk of) MI.
187
What are the side effects of warfarin?
Bleeding, bruising, anaemia, GI symptoms, vasculitis, purple staining of toes.
188
What are the interactions and contraindications of warfarin?
Contraindicated in conditions with high risk of bleeding, those undergoing surgery, risk of abortion. Risk of bleeding increased with given with other anti-coagulants or anti-platelets. Contraindicated with drugs that enhance coagulation such as vit K.
189
What is the MoA for menandione sodium bisulfate (vikasol)? What drug class is it in?
Prodrug of vitamin K. Vit K reduced to vit K hydroquinone a cofactor in the posttranslational gamma carboxylation of glutamic acid residue in proteins. These proteins include prothrombin (II), proconvertin (VII), Christmas factor (IX), stuart factor (X), protein C, S and Zv as Gas6 so an important mediator of clotting. Fat soluble vitamin.
190
What are the clinical indications for menandione sodium bisulfate (vikasol)?
Assists in the normal clotting of blood. Prevention and treatment of hypoprothrombinaemia, obstructive jaundice, celiac disease, dysenty, Crohn’s disease and haemorrhagic disease in new-borns.
191
What are the side effects of menandione sodium bisulfate (vikasol)?
Haemolytic anaemia, brain damage in large doses.
192
What are the interactions and contraindications of menandione sodium bisulfate (vikasol)?
Contraindicated in patients suffering from haemolytic anaemia. Also contraindicated in patients taking blood thinners such as warfarin. The counteracting effects increase the risk of DVT or PE.
193
What is the MoA for calcium chloride? What drug class is it in?
Calcium is involved in formation of bone tissue, coagulation, cardiac activity, transmission of nerve impulses, improves muscle contraction, reduces vascular permeability, excitation of the SNS by increasing excretion of adrenaline. Also forms insoluble compounds with magnesium salts, oxalic and fluoric acid.
194
What are the clinical indications for calcium chloride?
Used in allergic diseases, hypocalemia, lead colic, hyperkalaemia, overdose of magnesium salts.
195
What are the side effects of calcium chloride?
Chalky taste in the mouth, peripheral vasodilation, decreased BP, arrhythmia.
196
What are the interactions and contraindications of calcium chloride?
In those with hypercalcemia, renal failure, ventricular failure, sarcoidosis, electrolyte imbalance, respiratory acidosis, respiratory failure.
197
What is the MoA for diphenhydramine (dimedrol)? What drug class is it in?
H1 antagonist. As an inverse agonist it reverses these effects. Crosses the BBB inversely agonising the H1 receptors in the CNS suppressing medullary cough reflex. Similar to muscarinic receptors so diphenhydramine also acts as an antimuscarinic agent. It is also an intracellular sodium blocker so may have local anaesthetic properties. 1st generation antihistamine.
198
What are the clinical indications for diphenhydramine (dimedrol)?
Treats sneezing, rhinorrhoea, watery eyes, itching nose and throat, insomnia, pruritis, urticaria, insect bites, allergic rashes and nausea. Improves the reaction to blood or plasma. In combination with epinephrine to control anaphylaxis. Treats motion sickness. It is a competitive antagonist of muscarinic ACh receptors so has an anti-parkinson effect.
199
What are the side effects of diphenhydramine (dimedrol)?
Crosses the BBB inversely agonising the H1 receptors in the CNS leading to drowsiness. Can also cause dry mouth, nose and throat; as well as constipation, dry eyes and blurred vision.
200
What are the interactions and contraindications of diphenhydramine (dimedrol)?
Contraindicated in those with overactive thyroid, IOP, closed angle glaucoma, high BP, stenosing peptic ulcer, blockage of urinary bladder, enlarged prostate, inability to empty bladder and chronic idiopathic constipation.
201
What is the MoA for loratadine? What drug class is it in?
Binds to histamine H1 receptors (similar to diphenhydramine). Binds to different sites of the H1 GPCR favouring the inactive form (inverse agonist). Second generation antihistamines do not cross the BBB - do not cause sedation.
202
What are the clinical indications for loratadine?
Indicated in allergic rhinitis, wheal formation, urticaria and other allergic dermatologic conditions.
203
What are the side effects of loratadine?
Stomach pain, headache, dry eyes / mouth / throat, diarrhoea, liver damage / inflammation, tightness in the chest, fainting, seizures and thrombocytopaenia.
204
What are the interactions and contraindications of loratadine?
Contraindicated while also taking Ranexa. Caution should be exercised if the patient is taking amiodarone, darunavir or dasatinib.
205
What is the MoA for interferon alpha? What drug class is it in?
Induces host cell enzymes that inhibit viral RNA translation degrading viral m and tRNA.
206
What are the clinical indications for interferon alpha?
Chronic hepatitis B + C, genital warts caused by papilloma-virus, leukaemia (hairy cell / chronic myelogenous), kaposi sarcoma.
207
What are the side effects of interferon alpha?
Flu-like symptoms, GI disturbances, fatigue, mental depression, bone marrow suppression, weight loss, neurotoxicity, thyroiditis, heart failure.
208
What are the interactions and contraindications of interferon alpha?
Contraindicated in autoimmune diseases such as rheumatoid arthritis and autoimmune hepatitis as well as severe depression and psychosis. Major interactions with tramadol.
209
What is the MoA for methyluracil? What drug class is it in?
Immuno-stimulating agent. Normalises nucleic acid metabolism, accelerates cell regeneration processes in wounds, accelerates tissue growth. Has an anti-inflammatory effect. Treats leukopenia, agranulocytic tonsilitis, anaemia.
210
What are the clinical indications for methyluracil?
Indicated in the promotion of healing in slow healing wounds, prevents skin reaction in irradiation of neoplasms.
211
What are the side effects of methyluracil?
Allergic reactions, burning at place of application.
212
What are the interactions and contraindications of methyluracil?
Contraindicated in patients with hypersensitivity to methyluracil and when there is excessive granulation in the wound. In patients with leukaemia and malignant diseases of bone marrow.
213
What is the MoA for ambroxol? What drug class is it in?
Mucolytic agent. Expectorant. Stimulates serous cell in bronchial mucosa and increases content of mucous changing the disturbed ratio. There is activation of hydrolysing enzymes and release of lysosomes from Clara cells decreasing viscosity. Increases mucociliary sputum transport.
214
What are the clinical indications for ambroxol?
Acute and chronic diseases of the respiratory tract such as chronic bronchitis, bronchial obstructive syndrome, asthma as well as in respiratory distress syndrome in premies.
215
What are the side effects of ambroxol?
Nausea, vomiting, diarrhoea, abdominal pain, skin rash, urticaria, angioedema.
216
What are the interactions and contraindications of ambroxol?
Interacts with antitussive agents as sputum separation is reduced due to decreased cough reflex. Increases penetration of amoxicillin, doxycycline into bronchial secretion.
217
What is the MoA for glaucine? What drug class is it in?
Central acting antitussive. Prevents calcium entry into the cell preventing muscular contraction Also a dopamine receptor antagonist inhibiting PDE4 in bronchi.
218
What are the clinical indications for glaucine?
Antitussive in bronchial asthma, pleurisy, whooping cough, tuberculosis and lung cancer.
219
What are the side effects of glaucine?
Sedation, fatigue and hallucinations, hypotension, nausea.
220
What are the interactions and contraindications of glaucine?
Contraindicated in arterial hypotension, MI and overproduction of sputum. No known drug interactions.
221
What is the MoA for acetylcysteine? What drug class is it in?
Increases volume of sputum. Sulfhydryl groups break intramolecular and intermolecular disulfide bonds of acid mucopolysaccharides of sputum. The mucoproteins are depolarised decreasing the viscosity of sputum. Prevents depletion of glutathione (antioxidant) leading to detoxification.
222
What are the clinical indications for acetylcysteine?
Mucolytic agent and management of acetaminophen poisoning.
223
What are the side effects of acetylcysteine?
Headache, tinnitus, tachycardia, hypotension, bleeding, bronchospasm, dyspnoea, vomiting, diarrhoea, stomatitis, abdominal pain, nausea and pyrexia.
224
What are the interactions and contraindications of acetylcysteine?
Contraindicated in peptic ulcers in the acute phase, haemoptysis, pulmonary haemorrhage, lactation. Antitussives increases sputum congestion. With nitroglycerine can cause hypotension.
225
What is the MoA for famotidine? What drug class is it in?
III generation H2 receptor blocker. Suppresses HCl from parietal cells stimulated by histamine from enterochromaffin cells, gastrin from gastrin cells and ACh.
226
What are the clinical indications for famotidine?
Indicated in the treatment of gastric ulcers, GERD, for hyper-secretory conditions such as Zollinger-Ellison syndrome.
227
What are the side effects of famotidine?
Dry mouth, nausea, vomiting, bloating, diarrhoea, constipation, cholestatic jaundice, increased level of transaminases, headache, fatigue, tinnitus, muscle and joint pain, bronchospasm, fever, acne vulgaris and dry skin.
228
What are the interactions and contraindications of famotidine?
Contraindicated in pregnancy and lactation. Interacts with antifungals such as ketoconazole and other H2 blockers such as cimetedine and ranitidine.
229
What is the MoA for bisacodyl? What drug class is it in?
Increases secretion of mucus in the colon, accelerating and enhancing peristalsis. The action is due to direct stimulation of nerve ending in the mucous membrane in the colon. Laxative. Diphenylmethane derivative.
230
What are the clinical indications for bisacodyl?
Indicated in the relief of constipation due to hypotension and flaccid peristalsis of the colon. Used in preparation for surgical operations and radiological studies. Regulates stool with hemorrhoids proctitis and anal fissures.
231
What are the side effects of bisacodyl?
Colick like pain in the intestine, diarrhoea - leading to loss of lfuid and therefore weakness, seizures and hypotension.
232
What are the interactions and contraindications of bisacodyl?
Contraindicated in intestinal obstruction, strangulated hernia, inflammatory diseases of the abdominal organs, GI bleeding, uterine bleeding, spastic constipation. Decreases plasma concentration of digoxin.
233
What is the MoA for sodium picosulfate? What drug class is it in?
Contact laxative. Inhibits absorption of water and electrolytes. Increases secretion into the lumen. Hydrolysed by colonic bacterial enzyme (sulfatase) to form BHPM which directly stimulates colonic peristalsis.
234
What are the clinical indications for sodium picosulfate?
Indicated for cleansing of the colon as preparation for colonoscopy in adults.
235
What are the side effects of sodium picosulfate?
Diarrhoea, excessive loss of fluid and electrolytes, weakness, seizures, hypotension and abdominal pain.
236
What are the interactions and contraindications of sodium picosulfate?
Contraindicated in intestinal obstruction, restrained hernia, inflammatory disease involving the abdominal organs, uterine and GI bleeding, cystitis, pregnancy, severe dehydration and in children under 4. Broad spectrum antibiotics reduce the effect of sodium picosulfate, increased risk of electrolyte imbalance when used with diuretics or glucocorticoids, high doses of sodium picosulfate lead to decreased tolerance of cardiac glycosides.
237
What is the MoA for omeprazole? What drug class is it in?
Benzimidazoles - inhibits H+/K+ ATPase enzyme system by binding covalently to the cysteine residues via disulfide bridges on the alpha subunit of the pump. This inhibits gastric acid secretion. Raises pH inhibiting the growth of H.pylori.
238
What are the clinical indications for omeprazole?
Treats active duodenal ulcers, eradicates H.pylori, treats GERD and EE, Zollinger - Ellison diseases and treats pathologic hyper-secretory conditions in adults.
239
What are the side effects of omeprazole?
Hematuria, proteinuria, arthralgia, muscle weakness, myalgia.
240
What are the interactions and contraindications of omeprazole?
Contraindicated in chronic liver disease, childhood. Interacts with antibiotics such as ampicillin, anticoagulants, benzodiazepines, clopidegrel.
241
What is the MoA for loperamide? What drug class is it in?
Non-selective calcium channel blocker and binds to opioid mu-receptors. Inhibits peristaltic activity of circular and longitudinal muscles of the intestinal wall. This slows intestinal motility and increases water and electrolyte movement through the bowel wall.
242
What are the clinical indications for loperamide?
Symptomatic relief of nonspecific diarrhoea and chronic diarrhoea associated with inflammatory bowel disease or gastroenteritis. Also reduces volume of discharge from ilesotomies.
243
What are the side effects of loperamide?
Abdominal pain, bloating, nausea, constipation, dry mouth, increased fatigue, drowsiness, dizziness.
244
What are the interactions and contraindications of loperamide?
Intestinal obstruction, constipation, bloating, acute dysentery, ulcerative colitis, pregnancy and pseudomembranous colitis. Co-trimoxazole increases the bioavailability of loperamide. Not to be given when patient experiences diarrhoea caused by C.Diff. Naloxone can be used as the antidote.
245
What is the MoA for pancreatin? What drug class is it in?
Mixture of lipase, protease and amylase so breaks down fat, proteins and starches in the small intestine.
246
What are the clinical indications for pancreatin?
Replaces deficiency of pancreatic enzymes caused by cystic fibrosis, chronic pancreatitis. Associated with parenchyma destruction.
247
What are the side effects of pancreatin?
Diarrhoea, constipation, discomfort in the stomach, nausea, hyperuricosuria and increased level of uric acid in the blood plasma.
248
What are the interactions and contraindications of pancreatin?
Contraindicated in acute pancreatitis. When used with antacids containing calcium carbonate of magnesium hydroxide the effectiveness of pancreatin is decreased. Decreased iron absorption when used with iron preparations.
249
What is the MoA for aprotinin (contrycal)? What drug class is it in?
Inhibits serine proteases (trypsin, chromotrypsin and plasmin). Inhibits kallikrein which inhibits the formation of factor XIIa. Inhibits the intrinsic pathway and inhibits plasmin. This slows fibrinolysis.
250
What are the clinical indications for aprotinin (contrycal)?
Reduces perioperative blood loss and the need for transfusion (in coronary bypass for instance). Also used in shock and in deep traumatic tissue damage.
251
What are the side effects of aprotinin (contrycal)?
Arterial hypotension and tachycardia, conjunctivitis, bronchospasm, myalgia, psychotic reactions, hallucinations, nausea, vomiting.
252
What are the interactions and contraindications of aprotinin (contrycal)?
Contraindicated in DIC, in the second trimester of pregnancy and during lactation. When added to heparinised blood it will increase coagulation time. Inhibits action of alteplase. Slows metabolism of suxamethonium chloride as it inhibits pseudocholinesterase (this increases the risk of apnoea).
253
What is the MoA for lisinopril? What drug class is it in?
Angiotensin converting enzyme inhibitor that prevents the conversion of angiotensin I to II. This prevents constriction of coronary blood vessels. Causes vasodilation and increases levels of bradykinin. Also inhibits the conversion of angiotensin to angiotensin I by renin.
254
What are the clinical indications for lisinopril?
Treats acute MI, hypertension (can be given in combination of hydrochlorothiazide for hypertension).
255
What are the side effects of lisinopril?
Dry cough, hyperkalaemia, skin rash and hypotension and altered taste.
256
What are the interactions and contraindications of lisinopril?
Contraindicated in pregnancy due to risk of foetal malformations. Interacts with other ACE inhibitors.
257
What is the MoA for magnesium sulfate? What drug class is it in?
Magnesium necessary for transport fo sodium, calcium and potassium across the membrane. Slows rate of SA node impulse formation and prolongs conduction time along myocardial tissue.
258
What are the clinical indications for magnesium sulfate?
IV treats arrhythmias (fatal arrhythmia torsades de pointes and digoxin - induced arrhythmias.
259
What are the side effects of magnesium sulfate?
Circulatory collapse, hypothermia, flushing, drowsiness, increased sweating, hypocalcemia, hyperkalemia, confusion, respiratory paralysis.
260
What are the interactions and contraindications of magnesium sulfate?
Contraindicated when there is myocardial damage, hypermagnesemia and hypercalcemia. Serious interactions include doxycycline, tetracycline, lymecycline.
261
What is the MoA for amlodipine? What drug class is it in?
Calcium channel blocker. Reduces availability of calcium for smooth muscle contraction. Is an arteriolar vasodilator.
262
What are the clinical indications for amlodipine?
Treats variant angina caused by spontaneous coronary spasm.
263
What are the side effects of amlodipine?
Peripheral oedema, tachycardia, hyperemia of skin, nausea, abdominal pain, fatigue, drowsiness, pain in the limbs, skin rash, itching.
264
What are the interactions and contraindications of amlodipine?
Contraindicated in patients with severe arterial hypotension, left ventricular outflow obstruction, who are haemo-dynamically unstable. The dosage of simvastatin should be reduced while taking amlodipine. Diltiazem and ketoconazole increase the concentration of amlodipine.
265
What is the MoA for losartan? What drug class is it in?
Competetively prevents binding of angiotensin II to AT1 on vascular smooth muscle and the adrenal glands. Causes vascular smooth muscle relaxation and lowers blood pressure. Binds preferentially to AT1, if losartan binds to AT2 will cause vasoconstriction.
266
What are the clinical indications for losartan?
Treats hypertension and reduces the risk of stroke, left ventricular hypertrophy, treats diabetic nephropathy with elevated creatinine and proteinuria as well as hypertension.
267
What are the side effects of losartan?
Dizziness, orthostatic, hypotension, hyperkalemia, diarrhoea, increased ALT, headache, impaired renal function and myalgia.
268
What are the interactions and contraindications of losartan?
Contraindicated in pregnancy, lactation and in children under 18. Use with diuretics will cause hypotension. Risk of hyperkalemia is given with potassium-sparing diuretics. Indomethacin decreases effectiveness of losartan.
269
What is the MoA for atorvastatin? What drug class is it in?
Competitive inhibitor of HMG CoA reductase (rate limiting step in cholesterol synthesis). Increases number of LDL receptors internalising LDLs and increasing its catabolism.
270
What are the clinical indications for atorvastatin?
Lowers cholesterol level in all types of hyperlipidemia. Only affective in those with functioning LDL receptors.
271
What are the side effects of atorvastatin?
Elevated liver enzymes (liver failure) and myopathy
272
What are the interactions and contraindications of atorvastatin?
Contraindicated in renal insufficiency and in pregnancy and lactation. Also increases the affect of warfarin.
273
What is the MoA for glyceryl trinitrate (nitroglycerin)? What drug class is it in?
Converted to nitrites, then nitric oxide increasing cGMP. This leads to dephosphorylation fo the myosin light chain causing vascular smooth muscle relaxation.
274
What are the clinical indications for glyceryl trinitrate (nitroglycerin)?
Reduce myocardial oxygen demand following relief of symptoms of stable, unstable and variant angina.
275
What are the side effects of glyceryl trinitrate (nitroglycerin)?
Headache, postural hypotension, facial flushing, tachycardia.
276
What are the interactions and contraindications of glyceryl trinitrate (nitroglycerin)?
Contraindicated in shock, collapse, hypotension, increased intracranial pressure, ACG, toxic pulmonary oedema. PDE5 inhibitors such as sildenafil potentiate the action of the nitrates.
277
What is the MoA for digoxin? What drug class is it in?
Inhibits the Na-K ATPase (sodium pump). This increases intracellular sodium and increases calcium levels in myocardial cells increasing the force of contractility. Also stimulates the PSNS via the vagus nerve decreasing the heart rate and reducing norepinephrine release.
278
What are the clinical indications for digoxin?
Treats moderate heart failure, increases myocardial contraction in children diagnosed with heart failure, maintains control of ventricular rate in adult patients diagnosed with chronic atrial fibrillation. Should be administered with an ACE inhibitor.
279
What are the side effects of digoxin?
Anorexia, nausea, vomiting, blurred vision, arrhythmias/
280
What are the interactions and contraindications of digoxin?
Contraindicated in patients with hypokalaemia. If tachycardia occurs then an anti-arrhythmic drug must be administered with digoxin immune Fab. Digoxin levels are increased when used with verapamil, amiodarone, clarithromycin. Shoudl be used with caution when the patient is taking other drugs that slow AV conduction such as beta blockers and diltiazem.
281
What is the MoA for corglycon? What drug class is it in?
Cadiac glycoside - positive ionotropic effect. Inhibits Na+/K+ ATPase on cardiomyocytes. Increased sodium and decreased potassium intracellularly. Activating sodium calcium metabolism. Increased calcium increases strength of contraction. Negative chronotropic effect - increases sensitivity of of cardipulmonary baroreceptors, increases activity of vagus nerve = antiarrhythmic effect by decrease of impulse speed and elongation of the refractory period.
282
What are the clinical indications for corglycon?
Used in therapy of chronic heart failure (II - IV class) and treatment of tachsystolic form of AF and flutter.
283
What are the side effects of corglycon?
Increased sensitivity to glycosides, arrhythmias, AV block, drowsiness, confusion, headache, delirious psychosis, anorexia and thrombocytopenia.
284
What are the interactions and contraindications of corglycon?
Contraindicated with glycosidic intoxication, AV block, Wolf-Parkinson-White syndrome, pregnancy, lactation and intermittent complete blockade. Interacts with adrenomimetics (contributes to arrhythmias), anticholinesterases (enhance bradycardia), glucocorticoids (enhance side effects of glycosides, diuretics enhance effects of glycosides due to hypokalaemia).
285
What is the MoA for amiodarone? What drug class is it in?
Class III anti-arrhythmic. Blocks potassium currents and therefore repolarisation in III phase. Increases duration (and refractory period) of AP. This reduces excitability.
286
What are the clinical indications for amiodarone?
Indicated in the treatment of recurrent ventricular fibrilation and recurrent hemodynamically unstable ventricular tachycardia. N.B: Only used when other anti-arhythmics are not tolerated by the patient.
287
What are the side effects of amiodarone?
Also interferes with beta receptors, Na and Ca channels. Leads to hypotension, bradycardia, Torsades de pointes. Increases activity of peroxisomes proliferator-activated receptors leads to steatogenic changes in the liver and other organs. Also binds to thyroid receptor due to its iodine content and could cause hypothyroidism or thyrotoxicosis. Can also cause cough, SOB, pulmonary fibrosis, pleurisy, bronchospasm, GI disturbances, auditory hallucinations, depression, micro-detachment of the retina.
288
What are the interactions and contraindications of amiodarone?
Contraindicated in those with sinus bradycardia, CVD, SA blockade, AV block, hypokalaemia, arterial hypotension, hypothyroidism, thyrotoxicosis, pregnancy, lactation, sensitivity to iodine as well as amiodarone.
289
What is the MoA for hydrochlorothiazide? What drug class is it in?
Diuretic. Transported into epithelial cells of distal convoluted tubule by OAT transporters and then into the lumen by MRP4. Acts on proximal distal convoluted tubule inhibiting reabsorption of of water by SLC12A3 (as binding reduces the magnitude of the concentration gradient).
290
What are the clinical indications for hydrochlorothiazide?
Management of oedema caused by congestive heart failure, hepatic cirrhosis, nephrotic syndrome, glomerulonephritis, renal failure and corticosteroid / oestrogen therapy. Can also be used to manage hypertension.
291
What are the side effects of hydrochlorothiazide?
Nausea, vomiting, diarrhoea, orthostatic hypotension, tachycardia, hypokalemia, hypomagnesemia, hyponatremia, hyperglycaemia, weakness and fatigue.
292
What are the interactions and contraindications of hydrochlorothiazide?
Contraindication in severe renal failure, anuria, hepatic insufficiency, diabetes melitus, hypokalemia, hyponatremia, hypercalcemia, Addison's disease, pregnancy, lactation. Enhances the effect of antihypertensives and non-depolarising muscle relaxants. If given with CNS depressants can increase risk of orthostatic hypotension, Corticosteroids increase the risk of hypokalemia. ACE inhibitors enhance antihypertensive effect.
293
What is the MoA for furosemide? What drug class is it in?
Loop diuretic. Blocks Na and Cl reabsorption in the proximal convoluted tubule and the ascending loop of Henle. Inhibits NKCC2 co-transporter in the nephron preventing transport from lumenal to basolateral side for reabsorption. The leads to excretion of water and the ions. Also causes vasodilation, leading vessels to be less responsive to vasoconstrictors such as angiotensin II, decreases production of natriuretic hormones (reducing potential for vasoconstriction).
294
What are the clinical indications for furosemide?
Used for treatment of oedema caused by congestive heart failure, cirrhosis of liver, renal disease, nephrotic syndrome. Also manages hypertension. Can also be given IV to treat pulmonary oedema.
295
What are the side effects of furosemide?
Decreased BP, orthostatic hypotension, tachycardia, collapse, arrhythmia, MG, tetany, paresthesia, confusion, visual and hearing impairment, loss of appetite, dry mouth, thrist, nausea, vomiting, constipation, diarrhoea, cholestatic jaundice, oliguria, urinary retention, nephritis, cytopenias, hypovolemia, dehydration, arrhythmia.
296
What are the interactions and contraindications of furosemide?
Decreases secretion of uric acid so contraindicated in gout. Also contraindicated in glomerulonrephritis, narrowing and obstruction in the urinary tract, in those with electrolyte imbalances, hepatic failure, obstructive heart disease, hypotension, and MI. There may be increased nephrotoxicity when used with aminoglycosides, risk of hypokalemia increased when used with beta agonists and corticosteroids, effectiveness of hypoglycemic drugs is decreased as furosemide can increase glucose concentration. ACE inhibitors increase antihypertensive effect. NSAIDs suppress production of PGs leading to sodium retention reducing the diuretic effect and decreasing the hypertensive effect.
297
What is the MoA for spironolactone? What drug class is it in?
Potassium sparing diuretic. Competitively inhibits aldosterone dependant Na / K exchange channels in the distal convoluted tubule. This increases excretion of Na and water but retains potassium. The excretion of water also leads to an antihypertensive effect.
298
What are the clinical indications for spironolactone?
Indicated for the treatment of heart failure, management of oedema, primary hyperaldosteronism, add on therapy for hypertension and for nephrotic syndrome when fluid and sodium restriction are inadequate.
299
What are the side effects of spironolactone?
Ulceration fo the digestive tract, dizziness, drowsiness, increase in urea concentration, hypercreatinemia, hyperuricemia, metabolic acidosis / alkalosis, thromboctopenia, agranulocytosis, gynecomastia, dysmenorrhea, erectile dysfunction, amenorrhea, hirsutism, breast carcinoma.
300
What are the interactions and contraindications of spironolactone?
Contraindicated in patients with Addison's, hyperkalemia, hypercalcemia, hyponatremia, chronic renal failure, anuria, pregnancy, metabolic acidosis, menstrual irregularities. Should not be taken with antihypertensives or ACE inhibitors, potassium preparations or potassium sparing diuretics because these may increase the possibility of hyperkalemia.
301
What is the MoA for allopurinol? What drug class is it in?
Analog of purine (hypoxanthine), metabolised to oxypurinol inhibiting xanthine oxidase enzyme. Prevents synthesis of uric acid by preventing synthesis of xanthine from hypoxanthine. It also increases the use of xanthine for nucleotide synthesis. This leads to negative feedback on the production of purine. Also increases the excretion of xanthine and oxypurines in urine. As its concentration in plasma is below its limit of solubility the risk of crystalluria is reduced and also encourages the dissolution of tophi.
302
What are the clinical indications for allopurinol?
Manages symptoms of primary and secondary gout. In the the management of patients with leukemia undergoing cancer therapy elevating serum uric acid levels. In the management of recurrent calcium oxalate calculi.
303
What are the side effects of allopurinol?
May cause arterial hypertension, bradycardia and dyspeptic symptoms.
304
What are the interactions and contraindications of allopurinol?
Contraindicated in patients with impaired liver or kidney function, pregnancy and lactation. Enhances the effects of anticoagulants and hypoglycemic drugs. Salicylates reduce the activity of allopurinol.
305
What is the MoA for iodine solution? What drug class is it in?
Elemental iodine precipitates tissue proteins. Has antimicrobial properties. Has an irritating effect on tissue and in high concentrations has a cauterising effect.
306
What are the clinical indications for iodine solution?
Used for infectious, inflammatory skin lesions, injuries, wounds and myalgia. Also used for chronic tonsilitis, atrophic rhinitis, trophic and varicose ulcers, wounds, infected burns, fresh thermal and chemical burns.
307
What are the side effects of iodine solution?
May cause skin irritation and iodism (rhinitis, urticaria, Quincke's oedema, salivation, lacrimation and acne).
308
What are the interactions and contraindications of iodine solution?
Contraindicated in those with hypersensitivity to iodine, thyrotoxicosis and herpetiform dermatitis. It is incompatible with essential oils, ammonia solution, white sedimentary mercury (can be explosive). Antiseptic activity is weakened in the presence of fat, pus and blood.
309
What is the MoA for chlorhexidine? What drug class is it in?
Antiseptic / bactericidal. Used against gram negative and positive bacteria. C < 0.01% bacteriostatic; C > 0.01% bactericidal; C > 0.05% fungicidal; 0.01 - 1.0% virucidal against lipophilic viruses.
310
What are the clinical indications for chlorhexidine?
Treats wounds and burns. Disinfects patients skin (and used by surgeons to disinfect their hands before procedures). Also disinfects surfaces and devices. Used for bacterial and fungal diseases of mucous membranes in urology, obstetrics, dentistry (gingivitis, stomatitis, periodontitis), prevention of STDs (gonorrhea, syphillis, trichomoniasis, chlamydia, ureaplasmosis).
311
What are the side effects of chlorhexidine?
Allergic reaction, dry skin, itching, dermatitis, photosensitivity, staining of enamel, deposition of tartar, taste disturbances, burning (with vaginal used).
312
What are the interactions and contraindications of chlorhexidine?
Contraindicated in patients with hypersensitivity to chlorhexidine. Precipitates at pH greater than 8. Should not be used in combination with anionic compounds such as soap. Hard water reduces bactericidal properties. Incompatible with carbonates, chlorides, phosphates, borates, sulfates and citrates.
313
What is the MoA for hydrogen peroxide? What drug class is it in?
Antiseptic (oxidant). Has a haemostatic effect. When it makes contact with damaged skin or mucous membrane, active oxygen is released and mechanical purification and inactivation of organic substances occurs. It is not sterilising - only provides temporary decrease in number of microorganisms.
314
What are the clinical indications for hydrogen peroxide?
Washing and rinsing with stomatitis, tonsilitis, gynaecological diseases, small superficial wounds, small capillary bleeding, nosebleeds.
315
What are the side effects of hydrogen peroxide?
Burning sensation a time of treatment and possibility of allergic reaction.
316
What are the interactions and contraindications of hydrogen peroxide?
Contraindicated in those with known hypersensitivity to hydrogen peroxide. Is unstable in alkaline environments, in the presence of metal salts, complex radicals of certain oxidants as well as light and heat.
317
What is the MoA for potassium permanganate? What drug class is it in?
Antiseptic. Upon contact releases atomic oxygen. The oxides form albuminates (giving it astringent and cauterising effects). It has a deodorising effect. Is effective in the treatment of burns and ulcers. It neutralises some poisons so is used in gastric lavage when their is a case of poisoning.
318
What are the clinical indications for potassium permanganate?
Used to wash wounds, ulcers, burns, douching and washing in gynecological and urological practice, rinsing the mouth and throat with infectious and inflammatory diseases, used in gastric lavage when alkaloid poisoning occurs.
319
What are the side effects of potassium permanganate?
At high concentration can cause tissue irritation, increased sensitivity of tissues, and in patients with reduced acidity in the GI leads to hematotoxic effect (methemoglobinemia).
320
What are the interactions and contraindications of potassium permanganate?
Contraindicated in those with known hypersensitivity to potassium permanganate. Also potentially volatile when interacting with tannin, sugar, coal, alcohol, glycerin, organic acids, sulfur, sodium thiosulfate, sodium nitrate and reduced iron. Leads to halogen release when used with bromides, iodides and chlorides.
321
What is the MoA for ciprofloxacin? What drug class is it in?
Acts on bacterial topoisomerase II (DNA gyrase) and topoisomerase IV. It targets the alpha subunits of DNA gyrase preventing supercoiling of bacterial DNA which prevents replication. Bacteriostatic. Fluoroquinolone.
322
What are the clinical indications for ciprofloxacin?
Used in the treatment of complicated UTIs, Pseudomonas aeruginosa resp infections in patients with cystic fibrosis, invasive external otitis caused by P.aeruginosa, chronic gram negative bacillary osteomyelitis, eradication of salmonella typhi in carriers, gonorrhoea, bacterial prostatitis, cervicitis and anthrax.
323
What are the side effects of ciprofloxacin?
Major side effects include GI disorders, skin rashes, arthropathy, headache, dizziness, seizures.
324
What are the interactions and contraindications of ciprofloxacin?
Contraindicated in patients using other quinolone drugs as it can increase significant side effects (arterial hypotension, drowsiness), pregnancy and lactation. Interacts with theophylline (as P450 is inhibited) leading to toxicity of the latter in asthmatics.
325
What is the MoA for benzylpenicillin sodium? What drug class is it in?
Binds to specific penicillin – binding proteins inside the bacterial cell wall. Inhibiting the third and last stage of cell wall synthesis. Autolysins aid in cell lysis. Beta lactam antibiotic.
326
What are the clinical indications for benzylpenicillin sodium?
Treats severe infections such as septicaemia, meningitis, pericarditis, endocarditis and severe pneumonia. Affective against gram-positive as well as some – gram negative organisms such as Neisseria gonorrhoeae and Leptospira weilli.
327
What are the side effects of benzylpenicillin sodium?
CNS toxicity, interstitial nephritis, haemolytic anaemia, leukopenia, thrombocytopenia, coagulation disorders and diarrhoea increases risk of candidiasis.
328
What are the interactions and contraindications of benzylpenicillin sodium?
Probenacid reduces tubular secretion increasing concentration. If given with tetracyclines bactericidal effect is decreased.
329
What is the MoA for amoxicillin? What drug class is it in?
Inhibits penicillin binding protein 1, preventing glycosyltransferase and transpeptidase reaction blocking cross-linking of D-alanine and D-aspartic acid in the bacterial cell wall. Bacteria then upregulat autolytic enzymes. Bacteriocidal antibiotic.
330
What are the clinical indications for amoxicillin?
Treatment of susceptible bacteria in the ENT, GUT, skin and LRT. It is given in combination with omeprazole in the treatment of H.pylori, With metronidazole in chronic gastritis and ulcers. Given in combination with clavulanic acid to prevent destruction by beta-lactamase.
331
What are the side effects of amoxicillin?
In patients with chronic diseases superinfection may occur. With long term use can cause CNS dysfunction, when used with metronidazole causes GI disturbances.
332
What are the interactions and contraindications of amoxicillin?
Contraindicated in EBV infection, leukaemia, severe GI infections. Decreases effect of contraceptives, synergistic effect with bactericidal drugs and antagonism with bacteriostatic drugs. Enhances effect of anticoagulants. NSAIDs and diuretics reduce tubular secretion.
333
What is the MoA for doxycycline? What drug class is it in?
Wide spectrum bacteriostatic action as it supresses protein synthesis. Inhibits translation by binding to 16S rRNA portion of 30S ribosome preventing tRNA binding. This stops bacterial replication. Tetracycline antibiotic.
334
What are the clinical indications for doxycycline?
Treats gram-positive and negative aerobes and anaerobes. Used specifically in the treatment of rocky mountain spotted fever, typhus, Q fever, rickettsiealpox, tick fevers, RT infection (mycoplasma pneumoniae), lymphogranuloma venereum (chlamydia trachomatis), psittacosis (chlamydia psittaci), trachoma, uncomplicated urethral / endocervical / rectal infections and inclusion conjunctivitis (chlamydia tranchomatis), nongonococcal urethritis caused by ureaplasma urealyticum and replasing fever (borrelia recurrentis).
335
What are the side effects of doxycycline?
(GI symptoms) nausea, vomiting, anorexia, abdominal pain, diarrhoea, constipation, dysphagia, glossitis, esophagitis, increase in hepatic transaminases, alkaline phosphatase and bilirubin. (Haematological changed) neutropenia, thrombocytopenia, haemolytic anaemia. Can also cause an increase in residual nitrogen, candidiasis, intestinal dysbiosis and discolouration of teeth in children.
336
What are the interactions and contraindications of doxycycline?
Children under eight, porphyria, liver failure, leukopenia, lactation, myasthenia gravis. Interacts with preparations containing metal ions as it forms inactive chelates. Antibacterial effect decreases with barbiturate effect. Dose adjustment is required for anticoagulants due to alteration of microflora. Reliability of contraceptives is reduced.
337
What is the MoA for azithromycin? What drug class is it in?
Binds to 23S rRNA of 50S ribosome subunit. Inhibits the transpeptidation and translocation steps of protein synthesis and assembly. Broad spectrum macrolide antibiotic.
338
What are the clinical indications for azithromycin?
Bacterial exacerbation of COPD or sinusitis caused by H.influenza, M. catarrhalis, S. pneumoniae. Pneumonia caused by C / M / S. pneumoniae, H. influenza. Urethritis and cervicitis caused by C. trachomatis, N. gonorrhoeae. Pharyngitis / tonsilitis caused by S. pyogenes. Skin infections caused by S. aureus, S. pyogenes, S. agalactiae. Male chancres caused by H. ducreyi.
339
What are the side effects of azithromycin?
GI disturbances (however, generally well tolerated), cholestatic jaundice, ototoxicity (irreversible hearing loss).
340
What are the interactions and contraindications of azithromycin?
Contraindicated in patients with hepatic dysfunction, prolonged QT intervals (caution advised when prescribed for patients with (taking) proarrhythmic conditions (drugs). Eliminates spp of flora that inactivates digoxin leading to greater reabsorption and hepatic circulation.
341
What is the MoA for lincomycin? What drug class is it in?
Binds to 50S subunit of ribosome preventing peptide bond formation (and therefore transcription) preventing protein synthesis. Bacteriostatic but bactericidal in high concentration.
342
What are the clinical indications for lincomycin?
Treats staphylococcal, streptococcal and Bacteroides fragilis infections. Lincosamide drug.
343
What are the side effects of lincomycin?
GI disturbances, haemopoietic effects (leukopenia, neutropenia etc), impaired renal function, vaginitis, tinnitus, vertigo.
344
What are the interactions and contraindications of lincomycin?
Contraindicated in those with severe hepatic or renal failure, pregnancy and in the period of breastfeeding. Possibly responsible for antimicrobial antagonism when used with penicillins, cephalosporins. Synergy with aminoglycosides. Antidiarrheal drugs reduce effect of lincomycin.
345
What is the MoA for fluconazole? What drug class is it in?
Inhibits fungal CYP450 dependent lanosterol 14-alpha-demethylase. Converts lanosterol to ergosterol which is required for fungal cell wall synthesis. Methylated sterols will also accumulate in the cell membrane which arrests growth. Anti-fungal drugs. Azole drug.
346
What are the clinical indications for fluconazole?
Used in the treatment of vaginal yeast infections, systemic infections, oesophageal, oropharyngeal infections, UTI, peritonitis caused by candidal cryptococcal meningitis. Can be used as prophylaxis for those predisposed to candida infection (those undergoing chemotherapy).
347
What are the side effects of fluconazole?
CNS and GI disturbances, hypersensitivity, WBC-penia, anaemia, hepatotoxicity, increase in bilirubin, ALT, AST, jaundice, hepatitis, increased QT interval, arrhythmias, myalgia.
348
What are the interactions and contraindications of fluconazole?
Contraindicated in those taking drugs that increase the QT interval and that are metabolised by CYP3A4 (erythromycin, quinidine, astemizole). Interacts with warfarin.
349
What is the MoA for isoniazid? What drug class is it in?
Bacteriostatic in resting organisms / bacteriocidal in dividing. Passes freely into mammalian cells so can be used for intracellular organisms. Prodrug activated by bacterial enzymes and inhibits synthesis of mycolic acid (cell wall components of mycobacterium). It penetrates well into caseous tuberculosis lesions. It is an anti-tubercular drug.
350
What are the clinical indications for isoniazid?
Used against mycobacteria.
351
What are the side effects of isoniazid?
Side effects are dose dependent. Fever, hepatotoxicity, haematological changes, arthritic symptoms and vasculitis.
352
What are the interactions and contraindications of isoniazid?
In patients with G6PD deficiency can cause haemolytic anaemia. Decreases the metabolisms of anti-epileptic drugs such as phenytoin, ethosuximide and carbamazepine increases plasma concentration and toxicity of these drugs.
353
What is the MoA for rifampicin? What drug class is it in?
Inhibits DNA-dependent RNA synthesis by inhibiting DNA-dependent RNA polymerase. It binds to DDRPs beta subunit and blocks elongation. Blocks synthesis of the second and third phosphodiester bonds on the RNA backbone. Antibiotic drug.
354
What are the clinical indications for rifampicin?
Treats mycobacterium tuberculosis, leprae, avium complex and Legionnaires' disease.
355
What are the side effects of rifampicin?
GI disturbances, renal tubule necrosis, interstitial nephritis , acute renal failure, menstrual irregularities, staining red of secretions.
356
What are the interactions and contraindications of rifampicin?
Contraindicated in those suffering from jaundice, recent infectious hepatitis, renal dysfunction. Rifampicin induces liver enzymes and accelerates metabolism of theophylline, anticoagulants, hypoglycaemic drugs, contraceptives.
357
What is the MoA for acyclovir? What drug class is it in?
Converted to the monophosphate by viral thymidine kinase VTK. VTK more effectively phosphorylates acyclovir than the hosts enzyme so is only activated in the infected cells. Monophosphate is then converted to triphosphate inhibiting viral DNA polymerase. Antiviral. Guanosine derivative.
358
What are the clinical indications for acyclovir?
Used against varicella zoster infections, herpes simplex infections and given prophylactically in patients who are being treated with immunosuppressants or radiotherapy (as they are at risk of reactivation of a latent virus) and in individuals who suffer from frequent recurrence of HSV genital infections.
359
What are the side effects of acyclovir?
Local inflammation when given IV, renal dysfunction (though this reduced when infused slowly), nausea, headache and encephalopathy.
360
What are the interactions and contraindications of acyclovir?
Caution in pregnancy, breast-feeding, dehydration and renal failure.
361
What is the MoA for chingamine? What drug class is it in?
Inhibits heme polymerase in malarial trophozites preventing conversion to hemazoin. Plasmodium spp accumulate toxic heme. When protonated it increases pH preventing virus particles utilising cellular machinery for fusion.
362
What are the clinical indications for chingamine?
Treats P. vivax / malariae / ovale / falciparum and treats extraintestinal amebiasis.
363
What are the side effects of chingamine?
GI disturbances, seizures, clouding of cornea and visual impairment with prolonged use, myocardial damage, decreased BP, leukopenia.
364
What are the interactions and contraindications of chingamine?
Contraindicated in those with G6PD deficiency (haemolytic anaemia), retinopathy and epilepsy. Digoxin concentration increases. Cimetidine decreases excretion of chloroquine. Antacids disrupt absorption. Other antimalarials may have an antagonistic effect.
365
What is the MoA for metronidazole? What drug class is it in?
Activated by anaerobic organisms to a compound that damages DNA leading to apoptosis of the parasite. Bactericidal nitroimidazole antibiotic.
366
What are the clinical indications for metronidazole?
Antiprotozoal agent. Also affective against anaerobic bacteria (Bacteroides Clostridia spp) and some streptococci. Effective in therapy of pseudomembranous colitis. Important in treatment of serious anaerobic infections. Used against trophozoites of E.Histolytica. Drug of choice for invasive amoebiasis of the intestine or the liver.
367
What are the side effects of metronidazole?
It has a metallic bitter taste, GI disturbances, dizziness, headache, sensory neuropathy.
368
What are the interactions and contraindications of metronidazole?
Due to its disulfiram-like action patients should avoid alcohol. Contraindicated in pregnancy.
369
What is the MoA for mebendazole? What drug class is it in?
Causes degeneration of tegument and intestinal cell of the worm. Binds to colchicine-sensitive site of tubulin preventing polymerisation of microtubules. this prevents uptake of glucose. The function of the cellular machinery reduces ATP production. This immobilises the parasite and kills it.
370
What are the clinical indications for mebendazole?
Treats Enterobium vermicularis, Trichuris trichiuria, Ascaris lumbricoides and Ancylostoma duodenale. (Pinworm, whipworm and hookworms).
371
What are the side effects of mebendazole?
GI disturbances, CNS disturbances, haemopoetic changes, hematuria and cylindruria.
372
What are the interactions and contraindications of mebendazole?
Those who have impaired liver function, pregnancy, lactation. Reduces the need for insulin. Metabolic inducers reduce the concentration of mebendazole.
373
What is the MoA for dimercaptol (unithiol)? What drug class is it in?
Forms complexes with heavy metals preventing metallic binding of sulfhydryl-containing enzymes. Complexes are then excreted in urine. Sulfhydryl drug. Competitively binds to the heavy metals.
374
What are the clinical indications for dimercaptol (unithiol)?
Treatment of arsenic, gold and mercury poisoning, lead poisoning. Also used for alcohol withdrawal syndrome.
375
What are the side effects of dimercaptol (unithiol)?
Nausea, dizziness, tachycardia, pallor of the skin.
376
What are the interactions and contraindications of dimercaptol (unithiol)?
Contraindicated in people with severe diseases of the hepato-biliary system and arterial hypertension.
377
What is the MoA for methotrexate? What drug class is it in?
Converted to methotrexate polyglutamate by folypolyglutamate. Inhibits enzymes for nucleotide synthesis such as AICART. This prevents cell division. The accumulation of AICART ribonucleotide inhibits adenosine deaminase --> accumulation of ATP and adenosine in the ECS. Stimulates adenosine receptors triggering AI action.
378
What are the clinical indications for methotrexate?
Paediatric acute lymphoblastic leukaemia and polyarticular juvenile idiopathic arthritis. Treats gestational choriocarcinoma, chorioadenoma destruens, hydatiform mole, breast cancer, epidermoid cancer, mycosis fungoides, lung cancer, non-Hodgkin's, maintenance of acute lymphocytic leukaemia.
379
What are the side effects of methotrexate?
Prevents DNA synthesis so possible side-effects are many including various -penias, increased risk of infection due to immunosuppression, increased liver enzyme function, may cause diabetes melitus and other metabolic disorders.
380
What are the interactions and contraindications of methotrexate?
Contraindicated in patients with hematopoietic disorders, severe renal failure, severe liver failure, alcohol abuse. Many drugs increase the concentration of methotrexate and B12 vitamins reduce the effectiveness of methotrexate due to their conflicting effects.
381
What is the MoA for potassium / magnesium asparaginate (panangin / asparkam)? What drug class is it in?
Stabilises cellular membranes by normalising the levels of magnesium and potassium in the cells. Detoxification of ammonia or increase in the tricarboxylic acid-cycle flux (increased levels of ammonia and depleted levels of potassium and magnesium ions in the plasma are associated with fatigue).
382
What are the clinical indications for potassium / magnesium asparaginate (panangin / asparkam)?
Treats and prevents cardiac disruptions caused by electrolyte disturbances (low potassium and magnesium). Including congestive heart failure, heart attacks, disorders of cardiac rhythm and improves cardiac glycoside tolerability.
383
What are the side effects of potassium / magnesium asparaginate (panangin / asparkam)?
Side effects include hypotension due to AV blockade, paraesthesia, cramps, hyporeflexia, vomiting, nausea, diarrhoea, discomfort in the area of the pancreas, respiratory depression, increased levels of magnesium and potassium in the blood.
384
What are the interactions and contraindications of potassium / magnesium asparaginate (panangin / asparkam)?
Decreases absorption of tetracycline. When used in combination with ACE inhibitors or potassium sparing diuretics - level of potassium increases. Caution when prescribing for patients who suffer from arrhythmias, heart failure or MI.