The Ninety-Six Most Common Drugs For The Final Control Flashcards
What is the MoA for lidocaine? What drug class is it in?
Lidocaine cations bind to calcium ions channels, locking them in the open state preventing depolarisation. Prevents transmission and aborts generation. Amide group anaesthetic.
What are the clinical indications for lidocaine?
Local or regional anaesthetic by infiltration techniques (percutaneous injection or IV regional anaesthesia by central or peripheral nerve block)
What are the side effects of lidocaine?
Nervous agitation, loss of consciousness, respiratory paralysis, decreased BP, bradycardia, cardiac arrest and inhibition of myocardial function.
What are the interactions and contraindications of lidocaine?
Cimetedine and propranolol reduce hepatic clearance. Barbiturates, phenytoin and rifampicin reduce effectiveness by induction of microsomal liver enzymes. Sedatives increase CNS inhibition.
What is the MoA for articaine (ultracaine)? What drug class is it in?
Hydrolysed articaine binds to and blocks sodium channels preventing depolarisation. Thiophene derivative local anaesthetic.
What are the clinical indications for articaine (ultracaine)?
Infiltration and conduction anaesthesia in dentistry.
What are the side effects of articaine (ultracaine)?
Loss of consciousness, respiratory depression / paralysis, muscle tremor / twitching –> seizures. Decreases BP, heart failure, shock. Visual disturbances.
What are the interactions and contraindications of articaine (ultracaine)?
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.
What is the MoA for atropine sulfate? What drug class is it in?
Binds to and inhibits muscarinic ACh receptors. Alkaloid (derived from belladonna) anti-muscarinic agent.
What are the clinical indications for atropine sulfate?
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.
What are the side effects of atropine sulfate?
Dry mouth, tachycardia, constipation, difficulty urinating, photophobia etc (promotes SNS effects).
What are the interactions and contraindications of atropine sulfate?
Atropine absorption decrease when used with antacids. Anticholinergic effect increased when given with other anticholinergic drugs. Increased BP with phenylephrine. Reduced concentration of levodopa.
What is the MoA for pilocarpine hydrochloride? What drug class is it in?
Muscarinic agonist. Increases secretion by exocrine glands, causes miosis. Methylimidazole derivative drug.
What are the clinical indications for pilocarpine hydrochloride?
Treats radiation induced xerostomia. Treats acute glaucoma, COAG.
What are the side effects of pilocarpine hydrochloride?
Headache, follicular conjunctivitis with prolonged use, dermatitis of the eye lid, severe myosis.
What are the interactions and contraindications of pilocarpine hydrochloride?
Contraindicated in those with eye diseases where miosis would be undesirable such as iritis. Antagonist of m-anticholinergics such as atropine.
What is the MoA for neostigmine (proserine)? What drug class is it in?
Ani-cholinesterase inhibitor. Stimulates nicotinic and muscarinic receptors - therefore improves muscle contraction. Lowers IOP in OAG. Cholinergic group of drugs.
What are the clinical indications for neostigmine (proserine)?
Symptomatic treatment of myasthenia gravis (improves muscle tone).
What are the side effects of neostigmine (proserine)?
GI symptoms, miosis, loss of consciousness, headache, arrhythmias, AV block, decreased BP, SOB, respiratory depression.
What are the interactions and contraindications of neostigmine (proserine)?
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.
What is the MoA for suxamethonium chloride (succinylcholine / dithylin)? What drug class is it in?
Persistent depolarisation of NMJ as dithylin mimicks ACh but is not rapidly hydrolysed by acetylcholinesterase. Depolarising neuromuscular blocker.
What are the clinical indications for suxamethonium chloride (succinylcholine / dithylin)?
Used in surgical procedures where rapid but brief muscle relaxation is required - such as in intubation, endoscopies and ECT.
What are the side effects of suxamethonium chloride (succinylcholine / dithylin)?
Hyperkalaemia, decreased BP, arrhythmia, bradycardia, respiratory paralysis, increased IOP.
What are the interactions and contraindications of suxamethonium chloride (succinylcholine / dithylin)?
ACG, MG, Duchennes, pulmonary oedema, hyperkalaemia. Anticholinesterase inhibitors, bradycardia, decreases effectiveness of MG drugs.
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).
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.
What are the side effects of epinephrine?
Angina pectoris, reflex bradycardia / tachycardia, reflex hypotension, anxiety, headache, fatigue, nausea, vomiting, prostatic hyperplasia, hypokalaemia, hyperglycemia
What are the interactions and contraindications of epinephrine?
Contraindicated in hypertrophic obstructive cardiomyopathy, pheochromocytoma, pregnancy, lactation.
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).
What are the clinical indications for phenylephrine (mesatone)?
Injection treats hypotension. Ophthalmic preparation dilates pupils. Treats congestion. Topically treats haemorrhoids.
What are the side effects of phenylephrine (mesatone)?
Increases BP long term, tachycardia / reflex bradycardia.
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.
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.
What are the clinical indications for propranolol (anaprilin)?
Treats hypertension, angina pectoris, AF, MI, essential tremor, migraine, pheochromocytoma.
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.
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.
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.
What are the clinical indications for metoprolol?
Treats angina, heart failure, MI, AF, atrial flutter and hypertension.
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.
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.
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.
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.
What are the side effects of dobutamine?
Eosinophilia, tachycardia, hypertension, arrhythmias, vasoconstriction, MI, ST segment elevation, urge to urinate.
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.
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.
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.
What are the side effects of salbutamol (albuterol)?
Expansion of peripheral vessels, tachycardia, hypokalaemia and tremors.
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.
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.
What are the clinical indications for reserpine?
Treats hypertension.
What are the side effects of reserpine?
Bradycardia, increases symptoms of angina pectoris, urinary retention, weight gain, decreased libido.
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.
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.
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.
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.
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.
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.
What are the clinical indications for droperidol?
Used as an antiemetic (such as in surgical and diagnostic procedures). Acts on the chemoreceptor trigger zone.
What are the side effects of droperidol?
Dysphoria, drowsiness (post-operatively), hypotension and tachycardia, nausea, vomiting, loss of appetite.
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.
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).
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.
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.
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.
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).
What are the clinical indications for nitrazepam?
Treats short term insomnia.
What are the side effects of nitrazepam?
Fatigue, cognitive impairment, muscle weakness, change in libido.
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.
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.
What are the clinical indications for sodium valproate?
Treats focal and primary generalised epilepsy.
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.
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.
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.
What are the clinical indications for phenobarbital?
Treats seizures (sans absence seizures).
What are the side effects of phenobarbital?
Weakness, drowsiness, fatigue, ataxia, depression.
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.
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.
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.
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.
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.
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.
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.
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.
What are the interactions and contraindications of ketamine?
Contraindicated in hypertensive and stroke patients. Enhances action fo CNS depressants. Enhances muscle relaxant activity.
What is the MoA for ethyl alcohol? What drug class is it in?
GABA agonist.
What are the clinical indications for ethyl alcohol?
Methanol intoxification
What are the side effects of ethyl alcohol?
Intoxification, low BP, agitation, low blood sugar, nausea, vomiting, excessive urination
What are the interactions and contraindications of ethyl alcohol?
Brain operations, coma, diabetes, alcoholism, low BP, liver/renal probelms,
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).
What are the clinical indications for morphine hydrochloride?
Management of chronic severe pain. Depresses cough reflex.
What are the side effects of morphine hydrochloride?
Respiratory depression, dependence, addiction, tolerance, severe withdrawal symptoms, nausea, urinary retention, constipation, sedation, hypotension, dysphoria.
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.
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.
What are the clinical indications for trimeperidine (promedol)?
Management of chronic severe pain. Depresses cough reflex.
What are the side effects of trimeperidine (promedol)?
Nausea, vomiting, weakness, dizziness, euphoria, disorientation.
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.
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.
What are the clinical indications for fentanyl?
Short term analgesia and anaesthesia (induction and maintenance). Control of chronic pain.
What are the side effects of fentanyl?
Drowsiness, confusion, hallucinations, euphoria, muscle stiffness, bradycardia, nausea, vomiting, constipation, respiratory depression, urinary retention.
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.
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).
What are the clinical indications for naloxone?
Reversal of narcotic (respiratory) depression induced by opioids.
What are the side effects of naloxone?
Tachycardia, hypo/hypertension, ventricular fib, pulmonary oedema, nausea, vomiting, trembling, increased sweating.
What are the interactions and contraindications of naloxone?
Contraindicated in those with hypersensitivity to naloxone. Naloxone may decrease the antihypertensive effect of clonidine.
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.
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.
What are the side effects of acetylsalicylic acid (aspirin)?
Angioedema, bleeding, bronchospasm, GI disturbances, reye syndrome in under 16s and Stevens - Johnson syndrome.
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.
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).
What are the clinical indications for diclofenac sodium?
Treatment of pain and inflammation and pain in osteoarthritis, rheumatoid arthritis, akylosing spondylitis.
What are the side effects of diclofenac sodium?
Erythema, dermatitis, hypertension, nasal congestion, diarrhoea, constipation.
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.
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.
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).
What are the side effects of paracetamol?
Large doses deplete glutathione in liver. May cause hepatic necrosis.
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.
What is the MoA for celecoxib? What drug class is it in?
NSAID. Selective COX-2 inhibitor (reversible) reducing production of PGE2.
What are the clinical indications for celecoxib?
Treats rheumatoid arthritis, osteoarthritis, acute to moderate pain.
What are the side effects of celecoxib?
Headache, dyspepsia, diarrhoea, abdominal pain.
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.
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.
What are the clinical indications for meloxicam?
Symptomatic relief in arthritis, osteoarthritis, juvenile rheumatoid arthritis.
What are the side effects of meloxicam?
GI disturbances, hypertension, triggers cytopenia, gastrointestinal bleeding.
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.
What is the MoA for caffeine sodium benzoate? What drug class is it in?
Adenosine receptor antagonist.
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.
What are the side effects of caffeine sodium benzoate?
Agitation, anxiety, tremor, headache, tachypnea, tinnitus, insomnia, tachycardia, arrhythmias, hypertension, nausea, vomiting, nasal congestion.
What are the interactions and contraindications of caffeine sodium benzoate?
Contraindicated in those with anxiety disorders, hypertension, glaucoma and epilepsy. Stimulants should be avoided.
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.
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.
What are the side effects of piracetam?
Increased sexual activity, dyspeptic symptoms, abdominal pain, nervousness, agitation, anxiety, irritability.
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.
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).
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.
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.
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.
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.
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.
What are the side effects of fluoxetine?
Headache, sweating, anxiety, agitation, GI effects, weakness, sexual dysfunction, weight gain, sleep disturbance, hyponatremia.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
What are the side effects of glibenclamide?
Nausea, vomiting, constipation, diarrhoea, hypoglycaemia and weight gain.
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).
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.
