Year 2 Drugs List Flashcards

Question

Neprilysin inhibitors Drugs MoA Indications Side effects/interactions

Answer 1

* **Sacubitril (incombinatin with ARB)** Inhibits the breakdown of natriuretic peptide Indications: * Heart failure with reduced ejection fraction Side effects/interactions: * Hypotension * Hypoglycaemia

Answer 2

* **Bisoprolol** * **Atenolol (B1 cardioselective)** * **Propranolol (B1 and B2)** Competitive inhibitors of adrenaline and noradrenaline at beta-adrenergic receptors, inhibit sympathetic stimulation of heart muscle.(B1 antagonists selective for cardiomyocytes and contractility) by inhibiting cAMP cascade (PKA etc) which in cardiomyocytes drives contraction (opposite to bronchiolar smooth muscle) * Negative inotropes and chronotropes. * Reduce workload of the heart relieving oxygen demand. (reduced heart rate = reduced cardiomyocyte contractility) Indications: * Hypertension * Stable angina Side effects/interactions: * Bradycardia * Bronchospasm * Dizziness (hypotension) * Constipation * Interacts with NSAIDs and digoxin **Contraindicated in asthmatic patients**

Answer 3

* **Doxazosin** Selective alpha1 adrenergic receptor blocker in the bladder neck, urethra and prostate. Prevents sympathetic neurons from initiating smooth muscle contraction, causing relaxation which allows urinary flow. Vasodilator, decreases total peripheral resistance by inhibiting the postsynaptic alpha-1 receptors on vascular smooth muscle. Indications: * Hypertension * BPH * Urinary retention Side effects/interactions: * Dizziness * Headache * Nausea * Dry mouth * Constipation * Anxiety * Back pain * Coughing * Dyspnoea * Fatigue * Myalgia * Paraesthesia * Vertigo * Not to be given with hypotensive drugs

Answer 4

* **Amlodipine** * **Nifedipine** * **Diltiazem** * **Verapamil** Prevent opening of L-type voltage-gated calcium channels reducing influx of Ca2+ into cells. Reduced intracellular calcium has vasodilator effect on resistance vessels = reduced afterload. Causes dilation of coronary arteries increasing blood flow. Do not act on veins. Indications: * Hypertension * Stable angina Side effects/interactions: * Oedema * Ankle swelling * Palpitations * Not to be given with beta blockers or digoxin

Answer 5

* **Glyceryl trinitrate** * **Isosorbide mononitrate** Metabolised to release NO which diffuses into cell and stimulates soluble guanylate cyclase. Increases cGMP in vascular smooth muscle cells: * Drives dephosphorylation of myosin light chains via activation of MLC phosphatase. * Inhibits influx of Ca2+ into smooth muscle cytoplasm causing relaxation. Works on vascular smooth muscle of arteries and veins: * Venodilation: reduces cardiac preload (capacitance) * Arteriodilation: coronary artery vasodilation increases blood flow to myocardium * Moderate arteriolar dilation: reduces cardiac afterload Indications: * Acute angina pectoris * Heart failure Side effects/interactions: * Hypotension * Headache * Not to be given with antihypertensives

Answer 6

* **Adrenaline (alpha and beta)** * **Noradrenaline (alpha)** * **Dobutamine (beta)** Adrenergic stimulation increases inotropy. Adrenaline: Binds and stimulates cardiomyocyte B1-adrenergic receptors. Used in cardiac arrest to drive cardiac muscle contraction and restore heart function. Positive inotrope and chronotrope. Indications: * Cardiac arrest * Cardiogenic shock Side effects/indications: * Arrhythmia

Answer 7

* **Aspirin** Blocks the enzyme action of platelet COX enzyme which is required for the synthesis of thromboxane A2 (TXA2). Reduced TXA2 synthesis results in inhibition of platelet activation and thrombus formation. * **Clopidogrel** ADP receptor blocker: binds to and block the function of ADP receptors on platelet surfaces, inhibiting platelet activation and subsequent thrombus formation. Indications: * Primary and secondary relief for CVD * Anticoagulant prophylaxis Side effects/interactions: * Gastrointestinal irritation and bleeding * Not to be given with anticoagulants

Answer 8

* **Warfarin** Inhibition of epoxide reductase which results in inhibition of vitamin K pathway and vitamin K-dependent coagulation factors (VII, IX, X and prothrombin/FII) (1972) Indications: * Prophylaxis and treatment of VTE * Prophylaxis of stroke from AF Side effects/interactions * Abnormal bleeding * Drug interactions: NSAIDs, diuretics

Answer 9

* **Dabigatran** Competitive, reversible direct inhibition of thrombin. Indications: * Prophylaxis of VTE post surgery

Answer 10

* **Apixaban** * **Edoxaban** * **Rivaroxaban** Inhibition of factor Xa in the coagulation cascade Indications: * Prophylaxis of stroke from AF * VTE Side effects/interactions: * Abnormal bleeding

Answer 11

* **Dalteparin (LMWH)** * **Tinzaparin (LMWH)** * **Enoxaparin (LMWH)** * **Unfractionated heparins** Inactivation of thrombin and factor Xa by reversibly binding to and increasing activation of anti-thrombin III. Indications: * Prophylaxis of VTE and P.E * Treatment of existing clots (higher dose) Side effects/interactions: * Abnormal bleeding

Answer 12

* **Alteplase** * **Urokinase** * **Streptokinase** Activates plasminogen to plasmin for proteolytic breakdown of fibrin and fibrinogen to restore blood flow Indications: * Myocardial infarction * Ischaemic stroke Side effects: * Arrhythmias * Bleeding * Streptokinase can only be used once as an immune response is generated, memory B cells produce anti-streptokinase ABs.

Answer 13

* **Simvastatin** * **Atorvastatin** Inhibiton of malevolate pathway needed for cholesterol synthesis. Inhibit HMG-CoA Reductase (HMGCR) enzyme which reduces circulating cholesterol by: * Reducing intrinsic production of cholesterol * Promoting uptake of excess cholesterol by liver. Indications: * Treatment of HF without affecting BP * Hypercholesterolaemia * Risk of CVD and stroke Side effects/interactions: * Myalgia * Interacts with verapamil and macrolides

Answer 14

Mnemonic: 1a antiarrhythmic Does - disopyramide Quiet - quinidine 1 But Lets -Lidocaine 1 Calm Fluttery - Flecainide Pulses- Propafenone Class 1a: * **Disopyramide** * **Quinidine** Class 1b: * **Lidocaine** Class 1c: * **Flecainide** * **Propafenone** Voltage-sensitive sodium channel blockade. Prolongs QT interval and increases QRS duration. Indications: * Class 1a: Ventricular and supraventricular arrhythmias * Class 1b: CPR (given IV) * Class 1c: Paroxysmal atrial fibrillation and ventricular ectopic beats “pill in pocket” Side effects/interactions: * Oedema

Answer 15

* **Atenolol** * **Bisoprolol** * **Metoprolol** Beta-adrenergic receptor blockade reducing adrenergic effects on inotropy and chronotropy. Indications: * Prophylaxis of paroxysmal atrial tachycardia or fibrillation Side effects/interactions: * Hypotension * Bradycardia * Bronchospasm * Not to be given with NSAIDs or digoxin

Answer 16

* **Amiodarone** * **Dronedarone** * **Sotalol** (also has some beta blocker activity) Potassium channel blockade, also evidence of beta blocker and calcium channel blocker properties – prolong QT interval. Indications: * Supraventricular, nodal and ventricular tachyarrhythmias, atrial fibrillation * CPR (given IV) Side effects/interactions: * Nausea * Vomiting

Answer 17

* **Verapamil** * **Diltiazem** Cardiac calcium channel blockade- reduction of action potential and cardiac output. Indications: * Supraventricular tachycardia (esp paroxysmal SVT) Side effects/interactions: * Constipation (diltiazem) * Hypotension (verapamil)

Answer 18

* **Digoxin** Reduces contractility of AV node. Indications: * Atrial fibrillation * Congestive heart failure Side effects/interactions: * Fatigue * Nausea

Answer 19

* **Adenosine** Activates adenosine type 2 receptors - coupled to Gs protein --\> stimulates AC --\> increase in CAMP --\> protein kinase activation --\> KATP activation --\> which cause hyperpolarisation. Slows conduction through AV node. (plus smooth muscle relaxation --\> increase in coronary bloody flow). Indications: * Supraventricular tachycardia Side effects/interactions: * Nausea * Contraindicated in obstructive airway disease

Answer 20

* **Atropine** Blockade of vagal (parasympathetic) muscarinic acetylcholine receptors in the SA and AV nodes. Indications: * Bradycardia (emergency) Side effects/interactions: * Urinary retention

Answer 21

* **IV Mg sulfate** Unclear – possible alteration of Na+, K+ and Ca2+ ion balance via ion channels and transporters. Indications: * Emergency arrhythmia * Emergency asthma Side effects/interactions: * Electrolyte irregularities

Answer 22

* **Salbutamol** (short acting) * **Terbutaline** (short acting) * **Salmeterol** (long acting) * **Formoterol** (long acting) Cellular target: Bronchiolar smooth muscle cells Molecular target: Stimulation of B2-adrenergic receptors * Activation of B2AR activates G-protein * Increases activation of adenylate cyclase * Adenylate cyclase converts ATP to cAMP * Increased cAMP activates protein kinase A which: * Drives Ca2+ into intracellular storage vesicles away from cytoplasm. * Reduces activity of myosin light chain kinase = reduced muscle contraction * Dephosphorylation of myosin light chain = reduced muscle contraction * Reduced cytoplasmic Ca2+ levels reduce smooth muscle contraction resulting in bronchodilation. Indications: * Asthma * Reversible airway obstruction Side effects/interactions: * Tachycardia * Tremor * Cardiac arrhythmias * Interacts with diuretics

Answer 23

* **Ipratropium** (short acting) * **Tiotropium** (long acting) Blocks M3 muscarinic acetylcholine receptors preventing stimulating effects of ACh: * Inhibits activation of G-protein therefore inhibits activation of phospholipase C enzyme (PLC) * PLC therefore cannot release calcium from intracellular stores * Cytoplasmic Ca2+ levels do not rise therefore bronchiolar smooth muscle contraction does not increase (inhibits bronchoconstriction) * =Bronchiolar relaxation Indications: * Acute asthma * Bronchospasm in COPD Side effects/interactions: * Dry mouth * Constipation

Answer 24

* **Aminophylline** * **Theophylline** Inhibit phosphodiesterase enzymes (PDE) preventing it from inhibiting CAMP. CAMP levels maintained therefore protein kinase A enzyme activated which stores intracellular Ca2+ into storage vesicles. Reduced cytoplasmic Ca2+ results in less smooth muscle contraction so less bronchoconstriction Indications: * Acute asthma * Reversible airways obstruction Side effects/interactions: * Headache * Nausea * Cardiac arrhythmias * Seizures * Interacts with antidepressants and salbutamol

Answer 25

* **Beclomethasone** * **Prednisolone** * **Hydrocortisone** * **Fluticasone** Targets immune cells of the lungs: macrophages, T-lymphocytes, eosinophils. Activates glucocorticoid receptors which interact with selected nuclear DNA sequences and influences the expression of genes: * Repression of pro-inflammatory mediators: IL-3, IL-5, Th2 cytokines * Expression of anti-inflammatory products: secreted leukocyte peptidase inhibitor (SLPI), Lipcortin-1 and upregulation of B2 adrenoceptors. Indications: * Asthma * Allergic rhinitis Side effects/interactions: * Cough * Hyperglycaemia * Muscle wasting * Thinning skin * Osteoporosis * Increased risk of infection * Moon face (facial swelling) * Interacts with aspirin

Answer 26

* **Motekulast** * **Zafirlukast** Blockade of leukotriene receptors. Leukotrienes released from mast cell upon activation, normally binds to CysLT1 leukotriene receptor to: * Stimulate bronchiolar smooth muscle constriction * Bind to and recruit immune cells such as eosinophils by guiding eosinophil chemotaxis. Leukotriene receptor antagonists block CysLT1 receptors on smooth muscle and eosinophils blocking the above effects. Indications: * Asthma * Allergic rhinitis * (used as a preventor) Side effects/interactions: * Abdominal pain * Interacts with phenobarbital

Answer 27

* **Dornase alfa** Synthetic DNAse 1 – breakdown Cystic fibrosis of extracellular DNA to reduce sputum viscosity. Indications: * Cystic fibrosis

Answer 28

* **Pramipexole** * **Ropinirole** * **Rotigotine** Synthetic dopamine, act on dopamine receptors (primarily D₂) to replace lost dopamine Less overall improvement than levodopa, more psychiatric side effects. Indications: * Parkinson's disease * Esp younger patients to delay the need for levodopa * First line for initial treatment * Can be used with levodopa in later stages Side effects/interactions: * Psychiatric symptoms (due to action on mesocortical and mesolimbic pathways) * Confusion, agitation * Nausea and vomiting * Sudden onset sleep/ drowsiness * On-off effects * Hypotension * Tachycardia * Interacts with MAOIs

Answer 29

Dopamine precursor: crosses blood brain barrier and is metabolised into dopamine to replace that lost. Works on dopamine receptors to restore activity in the nigrostriatal pathway. Indications: * Parkinson's disease (use as late as possible) Side effects/interactions: * Psychiatric symptoms (due to action on mesocortical and mesolimbic pathways) * Confusion, agitation * Nausea and vomiting * Sudden onset sleep/ drowsiness * On-off effects * Hypotension * Interacts with MAOIs * Tachycardia

Answer 30

* **Selegiline** * **Rasagiline** Inhibition of levodopa breakdown in the CNS by monoamineoxidase-B meaning more is available to be converted into dopamine. Indications: * Parkinson's disease * Use alongside levodopa

Answer 31

* **Carbidopa** * **Benserazide** Prevents the breakdown of levodopa in the periphery by dopa-decarboxylase enzyme allowing more to cross the blood brain barrier and be converted into dopamine. Indications: * Parkinson's disease * Use in conjunction with levodopa

Answer 32

* **Entacapone** * **Tolcapone** Prevents breakdown of levodopa in the CNS by Catechol-O-methyltransferase (COM-T) so more is available to be converted to dopamine. Indications: * Parkinson's disease * Use alongside levodopa Side effects/interactions: * Nausea * Vomiting

Answer 33

* **Orphenadrine** * **Procyclidine** * **Trihexphenadyl** Inhibits cholinergic fibres from the striatum to the globus pallidus that moderate GABAergic cells and prevents them from inhibiting the direct pathway and increase effects of the indirect pathway. Indications: * Parkinson's disease (iatrogenic) * Muscle rigidity * Negate the side effects of anti-psychotics Side effects/interactions: * Can reduce the absorption of levodopa * Dry mouth * Constipation

Answer 34

* **Tetrabenazine** Inhibits VMAT2 (vesicular monoamine transporter) within basal ganglia, preventing transport of dopamine into presynaptic vesicles therefore less released into the synaptic cleft. Indications: * Huntington's chorea Side effects/interactions: * Affects all monoamines: 5-HT and NA * Can cause depression

Answer 35

* **Sertraline** * **Citalopram** * **Fluoxetine** Inhibition of 5-HT reuptake pump in synaptic cleft. Indications: * Depression * Generalised anxiety disorder Side effects/interactions: * Slow onset, can increase depressive symptoms initially * Nausea * Sleep disorders * Sexual dysfunction * Increased bleeding * Serotonin syndrome (increased 5-HT levels)- Emergency * Interacts with NSAIDs and lithium

Answer 36

* **Moclobemide** Increases 5-HT and noradrenaline levels by reversibly inhibiting enzymatic breakdown by monoamine oxidase A. Indications: * Depression Side effects/interactions: * Tachycardia * Also affects dopamine levels * DO NOT USE WITH TCAs/SSRIs * Interacts with cheese (contains tyramine) * Postural hypotension * Restlessness * Convulsions * Sleep disorders

Answer 37

* **Amitryptiline** * **Nortryptiline** * **Dosulepin** 5 main actions: * Therapeutic effects: * 5HT reuptake inhibitor * Noradrenaline reuptake inhibitor * Side effect causing: * A1 adrenoceptor antagonist * Postural hypotension * H1 receptor antagonist: * Sedation * M1 receptor antagonist * Cardiac dysrhythmia Indications: * Depression Other side effects: * Confusion * Mania

Answer 38

* **Venlafaxine** Inhibits the reuptake pumps of both 5-HT and noradrenaline Indications: * Depression

Answer 39

* **Raboxetine** Inhibition of the noradrenaline reuptake pump. Indications: * Depression

Answer 40

* **Agomelatine** Increases slow wave sleep to prolong sleep duration and reset sleep patterns. Indications: * Depression

Answer 41

* **Bupropion** Inhibition of the noradrenaline and dopamine reuptake pumps in the synaptic cleft. Indications: * Depression

Answer 42

* **Mirtazipine** Increase neurotransmitter release by inhibiting a2 receptors which normally slow transmitter release. Indications: * Depression Side effects/interactions: * Decreased vascular flow in extremities * Postural hypotension * Fatigue * Bronchoconstriction * Cardiac failure * Bradycardia * Sleep disorders * Impotence

Answer 43

* **Haloperidol** * **Chlorpromazine** Selective dopamine D2 receptor antagonists. Also affect M1, H1, alpha1 receptors. Low efficacy (30% non-responders) Indications: * Schizophrenia * Haloperidol: used for short term treatment of extreme or aggressive behaviour, rapid tranquilisation * Haloperidol: huntington's Side effects/interactions: * Blurred vision * Tremor * Extrapyramidal symptoms (result of altering activity of nigrostriatal pathways): * Dystonias * Akathisia * Parkinsonism * Sedation * Seizures * Hypotension * Hypothermia * Hypersensitivity * Chlorpromazine: agranulocytosis * Tardive dyskinesia from prolonged use (choreiform movements, grimacing, tongue protruding)

Answer 44

* **Olanzapine** Antagonism of D1, D2, D3 and D4 receptors in the brain, 5HT2A, 5HT2C, 5HT3 and 5HT6 receptors, alpha-1 adrenergic receptor, histamine receptor H1 and multiple muscarinic receptors. * **Risperidone** 5HT2A and Dopamine antagonist * **Quetiapine** Antagonism of dopamine type 2 (D2) and serotonin 2A (5HT2A) receptors * **Clozapine** 5HT2A and domapine antagonist * **Amisulpride** 5HT7 and Dopamine (D1 & D2) antagonist (mesolimbic pathway) Indications: * Schizophrenia Side effects/interactions: * Extrapyramidal symptoms * Hypotension

Answer 45

* **Lithium carbonate** MOA unclear Indications: * Bipolar disorder Side effects/interactions: * Tremor * Hypothyroidism * Interacts with NSAIDs and ACE-inhibitors

Answer 46

* **Donepezil** * **Galantamine** * **Rivastigmine** Reversible inhibition of acetylcholinesterase Indications: * Dementia (mild to moderate) * Alzheimer's disease Side effects: * Nausea * Vomiting

Answer 47

* **Memantine** VD blocker of NDMA receptors Indications: * Dementia (moderate to severe) * Alzheimer's disease Side effects/interactions: * Constipation * Hypertension

Answer 48

* **Lorazepam** * **Midazolam** * **Diazepam** * **Zolpidem** (benzodiazepine-like) * **Temazepam** GABA PAM (y subunit). Enhanced effects of GABA. Co-agonist (positive allosteric modulators) which bind to the y-subunit of the GABAA receptor to increase action of GABA. Reduces neuronal transmission by increasing chloride entry into the cell leading to hyperpolarisation and decreased likelihood of action potential firing. Indications: * Anxiety and related disorders * Epilepsy * Acute seizures * Temazepam: sedation Side effects/interactions: * Drowsiness * Dependence * Not to be given with sedatives

Answer 49

5-HT_1A partial agonist Indications: * Anxiety and related disorders

Answer 50

* **Zopiclone** GABA PAM (γ-subunit) Enhanced effects of GABA Indications: * Insomnia

Answer 51

* **Ethosuximide** T-type calcium channel blocker Indications: * Epilepsy: generalised absence seizures first line Side effects/interactions: * Do not use with macrolide antibiotics * Nausea * Blurred vision

Answer 52

* **Sodium valproate** * ****Generalised tonic-clonic seizures (first line) * Generalised abscence seizures (first line) * Generalised myoclonic seizures (first line) * Generalised abscence atypical, generalised tonic and generalised atonic seizures (first line) * **Lamotrigine** * Focal and focal to generalised seizures (first line) * Generalised tonic-clonic seizures (first line) * **Carbamazepine** * Focal and focal to generalised seizures (first line) Sodium channel blockers in inactivated state. Indications: * Epilepsy (see above) Side effects/interactions: * Sodium Valproate: Teratogenicity: foetal developmental defects * Cognitive impairment * Visual impairment * Peripheral neuropathy * Gum hyperplasia * Anaemia * Osteomalacia

Answer 53

* **Flumazenil** Antagonises GABA signalling Indications: * Reversal of benzodiazepine sedation

Answer 54

* **Phenobarbitone** * **Pentobarbitone** * **Primidone** Co-agonist of the GABA_Areceptor (B subunit) to increase activity. Reduces neuronal transmission by enhancing inhibition Indications: * Epilepsy/acute seizures * Anaesthesia/anxiolytic Side effects/interactions: * Dizziness/fainting * Drowsiness * Withdrawal on termination * Tolerance and dependency * Impaired motor coordination * Sedation * Impaired cognitive function * Retrograde amnesia * Interacts with sedatives and anticoagulants

Answer 55

Possible COX inhibitor, MoA unclear. Indications: * Mild-moderate nociceptive pain * Pyrexia Side effects/interactions: * Constipation * Interacts with warfarin

Answer 56

* **Ibuprofen** * **Diclofenac** * **Naproxen** * **Aspirin** Block production of prostaglandins by inhibiting cyclo-oxygenase enzyme: * COX1 : normal cell function * COX2 : inflammation * COX3 : fuck knows Inhibiting COX2 reduces production of inflammatory prostaglandins therefore reduce activation of prostanoid receptor and Na+ channel activation. Reduced Na+ channel activation leads to decreased depolarisation and less pain transmission. Indications: * Mild to moderate pain * Inflammation Side effects/interactions: Inhibiting COX1 inhibits production of PGE1 and PGI2 which have a role in normal physiological processes in platelets, endothelium, kidney, stomach and intestinal function. * Bleeding * Stomach ulcers * Heartburn * Nausea/ vomiting * Diarrhoea * Headache * Tinnitus * Hypertension * Interacts with ACE-inhibitors & diuretics

Answer 57

* **Eterocoxib** * **Celecoxib** COX-2 inhibition, localised prostaglandin blockade Indications: * Pain * Inflammation Side effects/interactions: * Less GI side effects than normal SAIDs * Indigestion * Avoid with NSAIDs and SSRIs

Answer 58

* **Codeine** * **Dihydrocodeine** Mimic endogenous opioids acting on opioid receptors µ, K, delta and ORL-1. Decrease neuronal transmission by: * Hyperpolarising the cell so it is less likely to fire AP when simulus arrives: * Decreases opening of voltage gated Na+ channels * Increases K+ outflow via KATP and KIR channels * Reduces exocytosis of transmitters * Decreases Ca2+ release from intracellular stores Indications: * Mild to moderate chronic and acute pain Side effects/interactions: * Constipation * Nausea * Drowsiness * Avoid giving with sedatives

Answer 59

* **Morphine** * **Diamorphine** * **Pethidine** * **Fentanil** Mimic endogenous opioids acting on opioid receptors µ, K, delta and ORL-1. Decrease neuronal transmission by: * Hyperpolarises the cell so it is less likely to fire when AP arrives: * Decreases opening of voltage gated Ca2+ channels * Increases K+ outflow via KATP and KIR channels * Reduces exocytosis of transmitter vesicles * Decreases Ca2+ release from intracellular stores Indications: * Severe pain * Cancer care, palliative care, coronary care Side effects/interactions: * Drowsiness * Respiratory depression * Constipation * Nausea * Tolerance and dependance/withdrawal * Avoid with sedatives

Answer 60

* **Buprenorphine** * **Pentazocine** Modulation of analgesic opioid receptors (agonist for u and antagonist for k) Indications: * Moderate to severe pain * Opioid addiction Side effects/interactions: * Constipation * Nausea * Avoid with sedatives

Answer 61

* **Naloxone (shorter half life)** * **Naltrexone (longer half life)** Competitive opioid receptor antagonist Indications: * Opioid overdose, respiratory depression Side effects/interactions: * Nausea * Constipation

Answer 62

* **Buprenorphine** µ agonist and k antagonist * **Methadone** µ agonist, narcotic opioid replacement Indications: * Opioid addiction Side effects: * Constipation * Nausea * Avoid with sedatives

Answer 63

* **Pregabalin** VDCC antagonist * **Gabapentin** VDCC antagonist * **Amitriptyline** See tricyclic antidepressants Indications: * Neuropathic pain Side effects/interactions: * Dizziness * Fatigue

Answer 64

* **Nitrous oxide** MoA unclear Indications: * Analgesia during childbirth Side effects/interactions: * Decreased vitamin B12 synthesis

Answer 65

* **Propofol (IV)**: MoA unclear * **Isoflurane (inhaled)**: MoA unclear * **Sevoflurane (inhaled)**: MoA unclear * **Ketamine (IV)** : NDMA receptor blockade Indications: * Induction of anaesthesia for major surgery * Propofol: maintenance of anaesthesia Side effects/interactions: * Decreased cardiac contractility * Respiratory depression (in overdose leading to respiratory failure and death) * Decreased CNS function * Reduced sympathetic activity

Answer 66

* **Lidocaine** * **Bupivicaine** * **Levobupivaine** Voltage-gated sodium channel blockade in 2 ways: * Directly entering open sodium channels (use-dependence, more channels open = bigger the effect) * Accessing sodium channels by crossing axonal membrane and binding from the inside Indications: * Local anaesthesia: * Lidocaine: regional IV anaesthesia, nerve block, dental and topical. * Bupivicaine/levobupivicaine: local infiltration, regional IV anaesthesia, epidural, peripheral nerve block, sympathetic block. Side effects/interactions: * Rash

Answer 67

* **Atracurium besolate** * **Vecuronium** Competitive antagonists of Ach receptors preventing depolarisation, blocking the effect of Ach. Also act presynaptically to reduce Ca2+ entry, reducing its release in vesicles into the synaptic cleft. 3-4 min time to max block, 40-45 min duration. Indications: * Tracheal intubation and mechanical ventilation during surgery Side effects/interactions: * No CNS side effects due to inability to cross BBB * Vecuronium has active metabolite that may produce residual paralysis * Hypotension * Skin flushing

Answer 68

* **Neostigmine** Non-competitive block of acetylcholinesterase (AchE) breakdown of Ach to increase levels of Ach in the junctional cleft. Causes muscle paralysis by overloading the system, activating all Ach receptors at maximum and leaving no room for additional movement; similar to depolarising NMBs. * **Suxamethonium** Rapid action, muscle relaxation within 1 minute: needs continuous infusion. Non-competitive agonists of ACh receptors causing prolonged depolarisation (causes receptor to close and repolarise despite receptor still being bound) and blockage of the receptor preventing further depolarisation and muscle contraction. Indications: * Tracheal intubation and ventilation during surgery * Relaxes muscles by blocking ACh at the NMJ Side effects: * Initial depolarisation causes fasciculations and increased likelihood of pain on recovery * Increase parasympathetic activity: * Bradycardia * Increased secretion and peristalsis

Answer 69

* **Neostigmine** Anticholinesterase Reverses the effects of non-polarising NMB but prolongs the effects of polarising NMB suxamethonium. * **Sugammadex** Selective relaxant binding agent, binds to the drug to form a complex, encapsulating and inactivating it and preventing it from working at the NMJ. Rapid action, rapidly cleared from plasma and excreted in urine No effect on the cholinergic nervous system, minimises risk of residual paralysis. Indications: * Sugammadex: Immediate reversal of NMB to reduce post-operative pulmonary compications * Neostigmine: reversal of non-polarising NMB. Also used in myasthenia gravis. Side effects/interactions: * Neostigmine: bradycardia due to muscarinic effects on PNS.

Answer 70

By binding to the presynaptic α-2 adrenoceptors in the brain, dexmedetomidine inhibits the release of noradrenaline, and terminates the propagation of pain signals. Activation of the postsynaptic α-2 adrenoceptors inhibits the sympathetic activity, decreasing blood pressure and heart rate. Indications: * Used as a sedative in intensive care if the patient needs to maintain verbal responsiveness. * Maintain sedation and relaxed muscle tone Side effects/interactions: * Bradycardia

Answer 71

* **Fentanil** * **Alfentanil** * **Remifentanil** Opioid receptor agonists Indications: * Maintenance of sedation and relaxed muscle tone * Fentanil: used for severe pain Side effects/interactions: * Respiratory depression * Constipation

Answer 72

* **Cyclizine** Histamine H₁ receptor blockade Indications: * Nausea * Vomiting Side effects/interactions: * Dry mouth * Sedation * High as a kite if taken IV

Answer 73

* **Domperidone** Dopamine D2 receptor blockade in the Chemoreceptor Trigger Zone. Indications: * Nausea and vomiting Side effects/interactions: * Cardiac disease

Answer 74

* **Benzylpenicillin** * **Amoxicillin**: LRTIs * **Coamoxiclav**: mixed infections e.g. dental abscesses and complicated LRTIs * **Penicillin**: tonsilitis * **Flucloxacillin**: SSTIs * **Piperacillin/tazobactam**: Complex LRTI Bacteriocidal, target bacterial cell wall- block cell wall synthesis causing cell lysis. Poor activity against intracellular organisms (e.g. legionella) or those with abnormal cell wall (e.g. chlamydia) Side effects/interactions: * Avoid use in patients with penicillin or cephalosporin induced anaphylaxis. * Rash/hypersensitivity * Interact with warfarin and methotrexate

Answer 75

* **Ceftriaxone** Bacteriocidal: cause cell lysis by blocking cell wall synthesis Indications: * Abdominal sepsis * Gram -ve infections * Bacterial meningitis * Orthopaedic infections Side effects/interactions: * Around 10% with penicillin allergy also have allergy to cephalosporins * Increased risk of CDAD * GI disturbances * Colitis * Interacts with warfarin

Answer 76

* **Meropenem** Bacteriocidal- block cell wall synthesis causing cell lysis. Indications: * Complex and multi drug resistant UTIs * Infections in intensive care * Hospital acquired septicaemia Side effects/interactions: * Abdominal pain * Pruritis

Answer 77

* **Trimethoprim** Inhibition of dihydrofolate reductase. Bacteriostatic. Indications: * UTI (uncomplicated) Side effects/interactions: * Rash * GI disturbances * Interacts with methotrexate * Contraindicated in pregnancy

Answer 78

* **Ciprofloxacin** Bactericidal if high dose: Inhibition of bacterial DNA gyrase enzyme, targets DNA structure and function. Indications: * Respiratory tract infections * Gram -ve infections excluding anaerobes * MRSA Side effects/interactions: * Nausea * Convulsions * Interacts with iron salts, NSAIDs

Answer 79

* **Erythromycin** * **Azithromycin** Bacteriostatic: target RNA and inhibition of bacterial protein synthesis. Indications: * LRTI * URTI * SSTI (in place of penicillins) * Atypical LRTIs (intracellular organisms) Side effects/interactions: * GI disturbance * Headaches * Interacts with digoxin, theophylline, statins

Answer 80

* **Doxycycline** Bacteriostatic: target RNA and inhibit bacterial protein synthesis Indications: * Atypical bacteria that lack the normal cell wall: * Chlamydia * Mycoplasmia * Rickettsia * e.g Typhus * CAP Side effects/interactions: * Use limited by GI intolerance * Photosensitivity

Answer 81

* **Nitrofurantoin** Interferes with bacterial DNA synthesis- bactericidal if high dose Indications: * Uncomplicated UTI Side effects/interactions: * Peripheral neuropathy

Answer 82

* **Gentamicin** Bactericidal if high dose: targets RNA, inhibition of bacterial protein synthesis Indications: * Severe gram -ve infections * Synergistic treatment for bacterial endocarditis * Opthalmic infection Side effects/interactions: * Use limited by renal toxicity and need for monitoring of drug levels

Answer 83

* **Vancomycin** Bactericidal: target bacterial cell wall in gram +ve bacteria Indications: * Multi drug resistant gram +ve cocci * E.g MRSA * C difficile infection Side effects/interactions: * Use limited by renal toxicity and need for monitoring of drug levels * Neutropenia * Renal impairment

Answer 84

* **Metronidazole** Bactericidal if high dose: inhibition of bacterial DNA synthesis Indications: * Anaerobic bacterial infections: * Leg ulcers * Pressure sores * Abscesses * Bacterial vaginosis Side effects/interactions: * Alcohol contraindicated

Answer 85

* **Isoniazid** Inhibition of bacterial cell wall synthesis * **Ethambutol** Inhibition of bacterial cell wall synthesis * **Rifampicin** Inhibition of mycobacterial RNA synthesis * **Pyrazinamide** Indications: * Tuberculosis Side effects/interactions: * Hepatotoxicity

Answer 86

* **Interferon alpha** Activation of antiviral intracellular and immune responses Indications: * Hepatitis B * Hepatitis C * Viral hepatitis from chronic CMB and EBV infections Side effects/interactions: * Flu-like symptoms * Loss of appetite * Fever * Lethargy * Depression * Secondary to night sweats -\> sleep deprivation

Answer 87

* **Aciclovir** * **Ganciclovir** Virus replication blockade. Aciclovir is converted to is triphosphate form (aciclovir triphosphate- ACV-TP) which competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain and inactivates the viral DNA polymerase. Indications: * Herpes simplex infection Side effects/interactions: * Nausea * Diarrhoea

Answer 88

* **Oseltamivir** Prevention of viral budding and infectivity Indications: * Influenza Side effects/interactions: * Nausea and vomiting

Answer 89

* **Ribavirin** Disrupts viral RNA synthesis Indications: * Hepatitis C * RSV

Answer 90

* **Tenofovir** Blockade of viral reverse transcriptase function for viral replication Indications: * HIV infection Side effects/interactions: * Rash * Steven-Johnson syndrome

Answer 91

* **Efavirenz** Blockade of viral reverse transcriptase function for viral genetic replication Indications: * HIV infection Side effects: * Rash * Steven-Johnson syndrome

Answer 92

* **Lopinavir** Blockade of viral protease required for virus particle assembly Indications: * HIV infection Side effects/interactions: * GI bleeding

Answer 93

* **Dolutegravir** Disrupts integration of HIV genome into host chromosomes Indications: * HIV

Answer 94

* **Enfuvirtide** Blockade of virus fusion to target cell membrane Indications: * HIV Side effects/interactions: * Pancreatitis

Answer 95

* **Maraviroc** Blockade of HIV binding to co- factor for cell entry Indications: * HIV Side effects/interactions: * Nausea * Diarrhoea

Answer 96

* **Fluconazole** Disruption of fungal membrane function Indication: * Candida infection Side effects: * Nausea * Abdominal pain

Answer 97

Increases uptake of glucose by cells Indications: * T1 & T2DM Side effects/interactions: * Hypoglycaemia * Interacts with digoxin, beta blockers

Answer 98

* **Metformin** Increases insulin sensitivity & inhibits hepatic gluconeogenesis Indications: * T2DM Side effects: * Nausea and vomiting * Interacts with digoxin, diuretics

Answer 99

* **Gliclizide** Stimulates pancreatic insulin secretion Indications: * T2DM Side effects/interactions: * Hypoglycaemia * Interacts with warfarin, NSAIDs

Answer 100

* **Pioglitazone** Increases insulin sensitivity in muscle and adipose tissue Indications: * T2DM Side effects/interactions: * Weight gain

Answer 101

* **Exenatide** Incretin analogue- improves glucose control Indications: * T2DM Side effects/interactions: * Asthenia

Answer 102

* **Sitaliptin** Reduces inactivation of incretins Indications: * T2DM Side effects/interactions: * Headache

Answer 103

* **Orlistat** Inhibition of GI uptake of dietary fat Indications: * Obesity, especially in the presence of T2DM Side effects: * Steatorrhoea * Faecal urgency

Answer 104

* **Levothyroxine sodium (T4)** * **Liothyronine sodium (T3)** Synthetic hormones to replace deficiency Indications: * Hypothyroidism Side effects/interactions: * Diarrhoea * Vomiting * Interacts with oral anticoagulants

Answer 105

* **Methotrexate** Inhibition of dihydrofolate reductase and DNA synthesis for lymphocyte proliferation Indications: * Rheumatoid arthritis * Broad spectrum of malignancies Side effects/interactions: * Nausea * Hair loss * Interacts with warfarin and corticosteroids

Answer 106

* **Azathioprine** MoA unclear Indications: * Rheumatoid arthritis * Crohn's disease Side effects: * Alopecia

Answer 107

* **Adalimumab** * **Infliximab** * **Etanercept** Blockade of TNF-alpha Indications: * Rheumatoid arthritis Side effects/interactions: * Infections

Answer 108

* **Sulfasalazine** * **Mesalazine** MoA unclear: possible COX inhibition; possible free radical scavenging, T cell suppression. Indications: * Rheumatoid arthritis * Crohn's disease Side effects/interactions: * Nausea * Interacts with digoxin, warfarin

Answer 109

* **Desogestrel and ethinyl-estradiol** Mimics ovulation, minimises LH and FSH. Indications: * Contraception * Polycystic ovary syndrome (PCOS) Side effects/interactions: * Weight gain * Depression * Increased DVT risk

Answer 110

* **Desogestrel** * **Levonorgestrel** (emergency contraception) Mimics ovulation, decreases LH and FSH, endometrial changes. Indication: * Hormonal contraception Side effects/interactions: * Depression

Answer 111

* **Etonogestrel** (subcutaneous implant) Mimics ovulation, decreases LH and FSH Indications: * Hormonal contraception Side effects: * Weight gain * Depression

Answer 112

* **Estradiol** * **Norethisterone** * **Medroxyprogesterone** Restores decreased hormone level and function Indications: * Menopause Side effects/interactions: * Weight gain * Depression

Answer 113

* **Dinoprostone** Prostaglandin E2: stimulates cervical ripening Indications: * Delay in labour

Answer 114

* **Oxytocin** Stimulates uterine contractions Indications: * Delayed labour Side effects/interactions: * Nausea * Arrhythmias

Answer 115

* **Misoprostol with mifepristone** Steroidal antiprogestogen in combination with synthetic prostadlandin Indication: * Medical termination of pregnancy Side effects: * GI cramps * Uterine contractions * Vaginal bleeding

Answer 116

* **Tranexamic acid** Inhibits fibrin clot breakdown by fibrin Indication: menorrhagia Side effects/interactions: * Nausea

Answer 117

* **Mefenamic acid** Inhibition of prostaglandin synthesis Indications: dysmenorrhoea Side effects/interactions: * GI bleeding

Answer 118

* **Tamsulosin** Smooth muscle relaxant acting on Alpha-1a adrenoceptors in the prostate and and alpha-1d adrenoceptors in the detrusor muscle. Indications: * BPH * Urinary retention Side effects/interactions: * Dizziness * Avoid with hypotensive drugs

Answer 119

* **Oxybutynin** Blockade of acetylcholine receptors leading to relaxation of smooth muscle in the bladder neck. Indications: * Overactive bladder Side effects/interactions: * Dry mouth * Tachy cardia preceded by transient bradycardia

Answer 120

* **Mirabegron** Stimulatin of Beta-3 adrenergic receptors, leading to relaxation of detrusor smooth muscle. Indications: * Overactive bladder Side effects/interactions: * Bladder pain

Answer 121

* **Finasteride** Inhibition of synthesis of dihydrotestosterone Indications: * BPH Side effects/interactions: * Impotence

Answer 122

* **Chloramphenamine** H₁ histamine receptor blockade Indications: * Hay fever * Urticaria Side effects/interactions: * Dry mouth * Sedation * Interacts with TCAs

Answer 123

* **Prednisolone** * **Hydrocortisone** * **Dexamethasone** Intracellular transcription factor interactions, gene expression Indications: * Suppression of inflammatory diseases: * Crohn's * RA Side effects/interactions: * Weight gain * Muscle atrophy * Interacts with oral antidiabetics

Answer 124

* **Cyclosporin** * **Tacrolimus** Inhibition of T cell signalling Indications: * Solid organ transplantation * Eczema (topical form) Side effects/interactions: * Hypertension * Interacts with aspirin

Answer 125

* **Cyclophosphamide** DNA crosslinking Indications: * Broad spectrum of malignancies Side effects/interactions: * Hair loss * Nausea * Bone marrow suppression

Answer 126

* **Paclitaxel** * **Docetaxel** Inhibition of microtubule assembly in the mitotic spindle Indication: * Broad spectrum of malignancies Side effects/interactions: * Hair loss * Nausea * Bone marrow suppression

Answer 127

* **Vincristine** * **Vinblastine** Inhibition of microtubule assembly in mitotic spindle Indications: * Broad spectrum of malignancies Side effects/interactions: * Hair loss * Nausea * Bone marrow suppression

Answer 128

* **Fluorouracil** * **Cytarabine** Inhibition of RNA and DNA synthesis Indications: * Broad spectrum of malignancies Side effects/interactions: * Hair loss * Bone marrow suppression * Nausea

Answer 129

* **Mercaptopurine** * **Thioguanine** Inhibition of DNA and RNA synthesis Indications: * Broad spectrum of malignancies Side effects/interactions: * Hair loss * Nausea * Bone marrow suppression

Answer 130

* **Doxorubicin** DNA intercalation; Inhibition of RNA and DNA synthesis Indications: * Broad spectrum of malignancies Side effects: * Hair loss * Bone marrow suppression * Nausea

Answer 131

* **Trastuzumab** Targets cells that overexpress Human Epidermal Growth Factor Receptor-2 (HER2) for tumour reduction and destruction. Indications: * Early breast cancer Side effects/interactions: * Fever * Chills

Answer 132

* **Rituximab** Targeted destruction of CD20+ B cells Indications: * Follicular lymphoma * Non-Hodgkins lymphoma Side effects/interactions: * Fever * Chills

Answer 133

* **Nivolumab** Stimulation of anti-tumour responses via blocking PD-1 Indications: * Melanoma Side effects/interactions: * Fever * Chills

Answer 134

* **Lenolidamide** Stimulation of T cell responses Indications: * Myeloma Side effects/interactions: * Foetal risk

Answer 135

* **Tamoxifen** Inhibition of oestrogen receptor function and cell proliferation in the breast Indications: * Breast cancer

Answer 136

* **Goserelin** Synthetic analogue of LHRH. Activates LHRH receptor function leading to sustained reduction in testosterone Indications: * Prostate cancer

Answer 137

* **Calcitonin** Inhibits mobilisation of calcium from bones Indications: * Osteoporosis * Hypercalcaemia Side effects/interactions: * Abdominal pain * Interacts with antacids

Answer 138

* **Alendronate** * **Pamidronate** Inhibits osteoclast function and bone resorption Indications: * Osteoporosis * Hypercalcaemia

Answer 139

* **IV calcium gluconate** * **Parathyroid hormone** * **Vitamin D** Restoration of calcium levels and metabolism Indications: * Hypocalcaemia * Bone loss

Answer 140

* Vitamin D * **Colecalciferol** * **Calcitriol** * **1,25-dihydroxy vitamin D** (usually only in the cases of advanced CKD) Restoration of vitamin D levels Indications: * Vitamin D deficiency

Answer 141

* **Raloxifene** Stimulation of oestrogen function in bone Indications: * Osteoporosis * Prevention of bone fractures Side effects/interactions: * Hot flushes * Interacts with warfarin

Answer 142

* **Denosumab** Inhibition of osteoclast function and bone resorption Indications: * Osteoporosis Side effects/interactions: * Hypocalcaemia

Answer 143

**Ferrous sulphate** Class: Oral iron compound Iron provision Indications: * Iron deficiency anaemia Side effects/interactions: * Constipation * Interacts with antacids (reduced absorption)

Answer 144

**Folic acid** Water soluble vitamin Supports nucleic acid synthesis Indications: * Folate-deficient anaemia

Answer 145

Watersoluble vitamin, enzyme cofactor Indications: * Pernicious anaemia

Answer 146

Mostly works on cardiac muscle. Slows Ca entry during phases 2 and 3 of cardiac action potential. * Moderate reduction in SVR by peripheral vasodilation * Moderate coronary vasodilation * Moderate decrease in cardiac contractility * Large reduction in heart rate * Mild reduction in stroke volume (Mild decrease in BP) Indications: HTN, tachyarrhythmias (esp re-entry and atrial origin) Side effects: * Heart failure * Heart block (esp when used with a B blocker) * Peripheral oedema * Constipation * Facial flushing * Headaches

Answer 147

Affects cardiac smooth muscle * Mild reduction in SVR through peripheral vasodilation * Moderate coronary vasodilation (useful for angina) * Moderate slowing of AV node- antiarrhythmic * Mild reduction in HR and stroke volume Mild decrease in BP Indications: HTN, arrhythmia, angina Side effects: * Facial flushing * Headaches * Peripheral oedema * Heart failure * Heart block

Answer 148

Amlodipine and Nifedipine * Large reduction in SVR by peripheral vasodilation * Moderat cardiac vasodilation * Mild decreased cardiac contractility * Moderate reflex increase in sympathetic tone * Mild slowing of AV node conduction * High increase in HR (compensatory from drop in BP) * Moderate natriuresis and diuresis Indications: HTN Side effects: * Marked facial flushing * Headaches * Peripheral oedema * Polyuria (exacerbate prostatism)