Drug of the Day

Question 1

Theophylline

Answer 1

Drug class: Phosphodiesterase Inhibitor/Adenosine Inhibitor

Common indications: Asthma

Other Important Drugs in Class: Aminophylline

Mechanism of action: Inhibits action of phosphodiesterase and adenosine, relaxing bronchial smooth muscle; inhibits T-Cell proliferation and cytokine production

Important adverse drug reactions: NV; Insomnia; Anxiety; Tachycardia; Arrhythmia

Contraindications: Serum levels should be monitored

Important drug-drug interactions: CYP1A2

Question 2

Sitagliptin

Answer 2

Drug class: DPP-4 Inhibitors/Glitptin

Common indications: T2DM

Mechanism of action: Prevents action of DPP-4 (to degrade Incretins/GLP-1), thus increasing Incretin action - ↑insulin secretion, increasing satiety.

Important adverse drug reactions: GI Upset; Pancreatitis (1%)

Contraindications: Pregnancy; Hx of Pancreatitis

Important drug-drug interactions: Other hypoglycaemic agents; Loop and Thiazide-like Diuretics (↑glucose reabsorption)

Question 3

Canagliflozin

Answer 3

Drug class: SGLT-2 Inhibitor/Gliflozin

Common indications: T2DM

Other Important Drugs in Class: Dapagliflozin

Mechanism of action: Inhibits SGLT-2, preventing glucose reabsorption

Important adverse drug reactions: UTI and genital infection; Thirst and polyuria; hypotension; WEIGHT LOSS

Contraindications: Hypovolaemia; Hypotension

Important drug-drug interactions: Antihypertensives; Antidiabetics

Question 4

Mesalazine

Answer 4

Drug class: Salicylate

Common indications: Ulcerative Colitis

Other Important Drugs in Class: Sulfasalazine

Mechanism of action: 5ASA inhibits prostaglandin synthesis and reduces migration of inflammatory cells in the bowel wall

Important adverse drug reactions: Nausea; Dyspepsia; Leukopenia

Contraindications: N/A

Important drug-drug interactions: N/A

Question 5

Warfarin

Answer 5

Drug class: Vitamin K Antagonist

Common indications: VTE; AFw/E; PE

Other Important Drugs in Class: N/A

Mechanism of action: Inhibits reduction of oxidised Vit K, preventing production of II, VII, IX, and X

Important adverse drug reactions: Bleeding

Contraindications: Pregnancy (Teratogen)

Important drug-drug interactions: CYP2C19; Highly protein bound (NSAIDs); Cephalosporins (eliminate Vit K production by bacteria)

Question 6

Protamine Sulphate

Answer 6

Drug class: ATIII Inhibitor

Common indications: Heparin Overdose

Other Important Drugs in Class: N/A

Mechanism of action: Inhibition of ATIII

Important adverse drug reactions: Clotting

Contraindications: N/A

Important drug-drug interactions: N/A

Question 7

Rituximab

Answer 7

Drug class: Anti-CD20

Common indications: RA; SLE; Lymphoma

Other Important Drugs in Class: N/A

Mechanism of action: Binds to CD20, found on acative B-cells, causing B cell apoptosis

Important adverse drug reactions: N/A

Contraindications: N/A

Important drug-drug interactions: N/A

Question 8

Insulin Dosing

Answer 8

Question 9

Tranexamic Acid

Answer 9

Drug class: Antifibrinolytic

Common indications: Bleeding

Other Important Drugs in Class: N/A

Mechanism of action: Prevents action of plasmin

Important adverse drug reactions: Clotting

Contraindications: N/A

Important drug-drug interactions: N/A

Question 10

Pioglitazone

Answer 10

Drug class: Thiazolidinediones/Glitazones

Common indications: T2DM

Other Important Drugs in Class: Rosiglitazone

Mechanism of action: Activates PPAR-Γ, which sensitises muscle and adipose tissue to insulin, decreases gluconeogensis

Important adverse drug reactions: GI upset; Fluid retention; Fracture Risk; Bladder Cancer; WEIGHT GAIN

Contraindications: Heart Failure (fluid retention)

Important drug-drug interactions: other hypoglycaemic agents

Question 11

Digoxin

Answer 11

Drug class: Class V Antiarrhythmic/Cardiac Glycoside

Common indications: HF; Fast AF

Other Important Drugs in Class: N/A

Mechanism of action: Increases vagal tone -> slows AVN conduction

Important adverse drug reactions: Arrhythmias; N+V; blurred/yellow vision

Contraindications: N/A

Important drug-drug interactions: Diuretics (hypokalaemia increases toxicity of digoxin); CYP3A4 inhibitors

Question 12

Losartan

Answer 12

Drug class: Angiotensin-II Receptor Antagonist

Common indications: Hypertension; Heart Failure; Diabetic Nephropathy

Other Important Drugs in Class: Candesartan

Mechanism of action: Antagonises AngII - decreases aldosterone and causes vasodilation

Important adverse drug reactions: Hypotensive Crisis; Hyperkalaemia (low aldosterone); Cause or worsen CKD/AKI

Contraindications: Renal Artery Stenosis; AKD; Pregnancy; CKD - Caution

Important drug-drug interactions: Potassium-increasing Drugs; NSAIDs

Question 13

Rivaroxaban

Answer 13

Drug class: Xa DOAC

Common indications: VTE

Other Important Drugs in Class: Apixaban; Edoxaban

Mechanism of action: Inhibit both free and bound Xa

Important adverse drug reactions: Bleeding

Contraindications: N/A

Important drug-drug interactions: CYP3A4

Question 14

Lactulose

Answer 14

Drug class: Osmotic Laxative

Common indications: Constipation

Other Important Drugs in Class: Movicol(Macrogol)

Mechanism of action: Draw fluid in (Lactulose); Retain the fluid they came with (Movicol/Macrogol)

Important adverse drug reactions: Cramping; Distention; Flatulence

Contraindications: N/A

Important drug-drug interactions: N/A

Question 15

Omeprazole

Answer 15

Drug class: Proton Pump Inhibitor

Common indications: Peptic Ulcer Disease; GORD; Dyspepsia

Other Important Drugs in Class: Lansoprazole

Mechanism of action: Irreversibly inhibits the proton pump, preventing gastric acid secretion

Important adverse drug reactions: GI Disturbance; Headache; Dizziness; Drowsiness

Contraindications: Osteoporosis

Important drug-drug interactions: CYP2C19; Can increase effects of Warfarin and Phenytoin

Question 16

Lisinopril

Answer 16

Drug class: Angiotensin Converting Enzyme Inhibitor

Common indications: Hypertension

Other Important Drugs in Class: Ramipril

Mechanism of action: Prevents conversion of Ang-I to Ang-II. Prevents Aldosterone release and peripheral Vasoconstriction. Supresses ADH, and potentiates Bradykinin

Important adverse drug reactions: CAPTOPRIL - Cough (Dry, Bradykinin); Angioedema (↑Afro-Caribbean); Proteinuria; Taste Disturbances/Teratogenic in 1st Trimester; Other (Fatigue, Headache); Potassium ↑; Renal Impairment; Itch; Low BP

Contraindications: Renal Artery Stenosis; AKD; Pregnancy; CKD; Idiopathic Angioedema

Important drug-drug interactions: ↑K drugs; NSAIDs; Other Hypotensives

Question 17

Levetiracetam

Answer 17

Drug class: Synaptic Vesicle Inhibitor

Common indications: Focal and Generalised Seizures

Other Important Drugs in Class: N/A

Mechanism of action: Stops release of neurotransmitters into synapse and reduces neuronal activity

Important adverse drug reactions: NV; Dizziness

Contraindications: N/A

Important drug-drug interactions: N/A

Question 18

Insulin

Answer 18

Drug class: Insulin

Common indications: Diabetes Mellitus

Other Important Drugs in Class: N/A

Mechanism of action: Replaces missing Insulin - binds to Insulin receptors

Important adverse drug reactions: Hypoglycaemia; Lipodystrophy

Contraindications: Hypoglycaemia; Renal Impairment

Important drug-drug interactions: Thiazides, Sterroids; Thyroid medications; Rifampin (increase insulin requirements); Alcohol, NSAIDs, Sulfonylureas, Warfarin (decrease insulin requirements); ß-blockers mask hypoglycaemia

Question 19

Levodopa

Answer 19

Drug class: Dopamine Precursor

Common indications: Parkinson Disease

Other Important Drugs in Class: N/A

Mechanism of action: Converted to dopamine in CNS

Important adverse drug reactions: NV; Psychosis; Tachycardia; Dyskinesia

Contraindications: N/A

Important drug-drug interactions: Pyridoxine increases breakdown; MAOi - risk of hypertensive crisis

Question 20

Bisoprolol

Answer 20

Drug class: ß-Adrenoceptor Blocker/Class II Antiarrhythmic

Common indications: Hypertension; SVT; Sinus Tachycardia

Other Important Drugs in Class: Labetalol; Metoprolol

Mechanism of action: Blocks NAd, causing ↓HR and ↓Contractility. Decreases Automaticity

Important adverse drug reactions: Bronchospasms; Heart Block; Raunaud’s; Lethargy; Impotence; Mask Tachycardia

Contraindications: Asthma; COPD; Haemodynamic Instability; Hepatic Failure

Important drug-drug interactions: Non-dihydropyridine CCBs (can causes asystole)

Question 21

Aprepitant

Answer 21

Drug class: Neurokinin-1 RAntagonist

Common indications: Antiemesis (Chemotherapy)

Other Important Drugs in Class: N/A

Mechanism of action: Prevent action of substance P at CTZ; boosts effects of 5HT3R Antagonist; Anxiolytic and Antidepressant

Important adverse drug reactions: Headache; Diarrhoea; Stevens-Johnson

Contraindications: N/A

Important drug-drug interactions: N/A

Question 22

Infliximab

Answer 22

Drug class: Anti-TNFα mAb

Common indications: RA; Psoriasis; IBD

Other Important Drugs in Class: Adalimumab

Mechanism of action: Inhibits TNFα - reduces inflammation, angiogenesis, and joint destruction

Important adverse drug reactions: Reactivation of TB

Contraindications: Latent TB

Important drug-drug interactions: N/A

Question 23

Furosemide

Answer 23

Drug class: Loop Diuretic

Common indications: Fluid overload in HF; Acute Pulmonary Oedema; Nephrotic Syndrome

Other Important Drugs in Class: Bumetanide

Mechanism of action: Block N/K/2Cl, increasing Sodium and Water loss. (Sodium reabsorption increased later along the nephron, compensated by K loss)

Important adverse drug reactions: Dehydration; Hypotension; Hypokalaemia; Hyponatraemia; Hyperuricaemia; Arrhythmia; Tinnitus; ↑Cholesterol and Triglyceride

Contraindications: Hypokalaemia; Hyponatraemia; Gout; Hepatic Encephalopathy

Important drug-drug interactions: Aminoglycosides (both Ototoxic); Digoxin; Lithium (retains lithium)

Question 24

Montelukast

Answer 24

Drug class: Leukotriene Receptor Antagonist

Common indications: Long Term Asthma control; Asllergic Rhinitis

Other Important Drugs in Class: N/A

Mechanism of action: Blocks LK1R, preventing airway inflammation and bronchoconstriction

Important adverse drug reactions: Headache; GI distrubance; Hyperactivity; Dry Mouth

Contraindications: N/A

Important drug-drug interactions: N/A

Question 25

Ivabradine

Answer 25

Drug class: Class V Antiarrhythmic Common indications: Sinus Tachycardia (often in HF and angina) Other Important Drugs in Class: N/A Mechanism of action: Blocks I*f* channels, reducing SAN firing Important adverse drug reactions: N/A Contraindications: Pregnancy (teratogen) Important drug-drug interactions: N/A

Question 26

Selegiline

Answer 26

Drug class: Monoamine Oxidase B Inhibitor Common indications: Parkinsons Disease Other Important Drugs in Class: Rasagaline; Safinamide Mechanism of action: Inhibitor MAOB, preventing dopamine degradation Important adverse drug reactions: Nausea; Psychosis Contraindications: N/A Important drug-drug interactions: Opiods; SSRIs; Tricyclics

Question 27

Oestradiol

Answer 27

Drug class: Oestrogen Receptor Agonist Common indications: HRT; Contraception; Primary Osteoporosis Other Important Drugs in Class: Premarin Mechanism of action: Activates ER - stimulates growth of endometrium and breast, stimulates PR production; decreases bone resorption Important adverse drug reactions: Breast Tenderness; Thromboembolism; Impaired glucose tolerance; Endometrial cancer; Ovarian cancer; Breast cancer Contraindications: Ovarian, Breast, or Endometrial malignancy; Hx of thromboembolism or CAD Important drug-drug interactions: Other medications that increase thromboembolism

Question 28

Fondaparinux

Answer 28

Drug class: Synthetic ATIII Agonist Common indications: VTE Other Important Drugs in Class: N/A Mechanism of action: Activates ATIII, inhibiting Xa Important adverse drug reactions: Bleeding Contraindications: N/A Important drug-drug interactions: N/A

Question 29

Ispaghula Husk

Answer 29

Drug class: Bulk Forming Laxative Common indications: Constripation Other Important Drugs in Class: Methylcellulose Mechanism of action: Fibre Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions: N/A

Question 30

Alteplase

Answer 30

Drug class: Fibrinolytic Common indications: Acute Ischaemic Stroke Other Important Drugs in Class: Streptokinase Mechanism of action: Increases plasmin production (tPA/Streptokinase) Important adverse drug reactions: Bleeding Contraindications: N/A Important drug-drug interactions: Antiplatelets and anticoagulants

Question 31

Celecoxib

Answer 31

Drug class: COX-2 Inhibitor/NSAID Common indications: OA; RA Other Important Drugs in Class: Etoricoxib Mechanism of action: Inhibitor of COX-2, with less COX-1 action. Does not share antiplatelet action Important adverse drug reactions: Decreased GFR; Peptic Ulceration; Worsens IBD Contraindications: N/A Important drug-drug interactions: N/A

Question 32

Codeine

Answer 32

Drug class: Opiod Moderate Agonist Common indications: Pain; Cough; Diarrhoea Other Important Drugs in Class: N/A Mechanism of action: Converted into Morphine by CYP2D6; activates µ-Opiod R Important adverse drug reactions: Respiratory Depression (worse in children); Constipation Contraindications: Hepatic Failure; Respiratory Distress; Raised ICP; Opiod Use Important drug-drug interactions: Fluoxetine (CYP2D6 inhibitor)

Question 33

Cyclizine

Answer 33

Drug class: H1R Antagonist Common indications: Antiemesis (motion sickness, morning sickness) Other Important Drugs in Class: Promethazine; Diphenhydramine Mechanism of action: Inhibits Vestibular Nuclei and CTZ Important adverse drug reactions: Sedation; Excitation; Antimuscarinic; Cardiac Toxicity Contraindications: Extremes of age Important drug-drug interactions: N/A

Question 34

Tiotropium

Answer 34

Drug class: Long Acting Muscarinic Antagonist Common indications: Severe Asthma and COPD Other Important Drugs in Class: Ipratropium (SAMA) Mechanism of action: Antagonises mAChR, preventing broncoconstriction Important adverse drug reactions: Cough; Nasal Dryness and Irritation Contraindications: N/A Important drug-drug interactions: N/A

Question 35

Morphine

Answer 35

Drug class: Opiod Strong Agonist Common indications: Pain; Diarrhoea Other Important Drugs in Class: Fentanyl Mechanism of action: Activates µ-Opiod R; causes Histamine release (less in fentanyl) Important adverse drug reactions: Respiratory Depression; Vomiting; Miosis (all less in fentalyl) Contraindications: Asthmatics (W); Hepatic Failure; Respiratory Distress; Raised ICP; Opiod Use Important drug-drug interactions: N/A

Question 36

Trihexyphenidydyl

Answer 36

Drug class: Central Anticholinergic Common indications: Parkinsons Disease Other Important Drugs in Class: Orphenadrine; Procyclidine Mechanism of action: Blocks cholinergic receptors in basal ganglia Important adverse drug reactions: Urinary retention; Dry mouth; Constipation Contraindications: N/A Important drug-drug interactions: Other anticholinergics

Question 37

Ibuprofen

Answer 37

Drug class: Non-selective Non-Steroidal Anti-Inflammatory Drug Common indications: Inflammatory Disorders; Pyrexia; Pain Other Important Drugs in Class: Naproxen Mechanism of action: Anti-inflammatory Important adverse drug reactions: GI Irritation; GI Bleeding; Haemorrhage; Hypersensitivity; Reduces GFR Contraindications: Hypersensitivity; 3rd Trimester (closes DA) Important drug-drug interactions: ACEi; ARBs; Diuretics

Question 38

Pramipexole

Answer 38

Drug class: Dopamine Receptor Agonist Common indications: Parkinsons Disease Other Important Drugs in Class: Apomorphine; Ropinirole; Rotigotine Mechanism of action: Agonises D2R in basal ganglia Important adverse drug reactions: NV; Dizziness; Psychosis; Impusle Control Disorders Contraindications: Psychosis; Impulse Control Disorder Important drug-drug interactions: Dopamine Antagonist

Question 39

Diltiazem

Answer 39

Mix of Dihydropyridine and Phenylalkylamines

Question 40

5-Flurouracil

Answer 40

Drug class: Pyrimidine Antimetabolite Common indications: Cancer Other Important Drugs in Class: N/A Mechanism of action: Inhibits thymidylate synthetase, stopping cell growth Important adverse drug reactions: Vomiting; Stomatitis; Alopecia; anaemia; leukopenia Contraindications: N/A Important drug-drug interactions: N/A

Question 41

Tamoxifen

Answer 41

Drug class: ER Antagonist and Partial Agonist Common indications: ER+ Breast Cancer Other Important Drugs in Class: Clomifene (for treating infertility - promotes ovulation by ↑GnRH) Mechanism of action: Inhibits ER in breast tissue, suppressing breast tumour growth Important adverse drug reactions: Nausea; Hot flushes; Menstrual Irregularities; ↑risk of stroke, PE, and Uterine Cancer Contraindications: Pregnancy; Lactation Important drug-drug interactions: Oestrodiol

Question 42

Treatment Path for Hypertension

Answer 42

Step 1: HTN w/ T2DM - ACEi or ARB HTN w/o T2DM, \<55 and not Black - ACEi or ARB HTN w/o T2DM, \>55 - CCB HTN w/o T2DM, Black - CCB Step 2: Original + (other class or Thiazide) Step 3: ACEi or ARB + CCB + Thiazide Step 4: K \>4.5 - + α- or ß-Blocker K \> 4.5 - MRA

Question 43

Metformin

Answer 43

Drug class: Biguanide Common indications: T2DM Mechanism of action: Decreases Hepatic Gluconeogensis (but not all). Increases insulin sensitivity. Exclusively excreted by kidneys Important adverse drug reactions: GI Upset Contraindications: Stage 4 or 5 CKD (\<30 eGFR); Alcohol Intoxication Important drug-drug interactions: ACEi or NSAIDs (impair renal function); Loop and Thiazide-like Diuretics (↑glucose reabsorption)

Question 44

Cyclophosphamide

Answer 44

Drug class: Alkylating Agent Common indications: NH Lymphoma; myeloma; Leukaemia; RA; SLE Other Important Drugs in Class: N/A Mechanism of action: Cross-links DNA by bonding to guanine residues; prevents DNA replication and transcription. PRODRUG - converted by CYP2C19 to active Important adverse drug reactions: Haemorrhagic Cystitis (prevented by using aggressive hydration and/or Mesna); Risk of cancers; Infertility Contraindications: N/A Important drug-drug interactions: CYP2C19

Question 45

Buprenorphine

Answer 45

Drug class: Mixed Opiod Agonist/Antagonist Common indications: Pain; Opiod Addiction Other Important Drugs in Class: N/A Mechanism of action: High affinity for µR but low E(max); Antagonist at kR Important adverse drug reactions: Respiratory Depression; Hypotension; Nausea; Dizziness Contraindications: Hepatic Failure; Respiratory Distress; Raised ICP Important drug-drug interactions: N/A

Question 46

Amiodarone

Answer 46

Drug class: Class III Antiarrhythmic Common indications: Most arrhythmias (last line) Other Important Drugs in Class: Sotalol Mechanism of action: Blocks K+, Na+, Ca2+, and ß-receptors; increases refractory period; decreases Phase 0 speed; increases threshold; decreases phase 4; decreases speed of AV conduction Important adverse drug reactions: in long term use - Pulmonary fibrosis, hepatitis, increases LDL; optic neuritis; photosensitivity; thyroid disease Contraindications: N/A Important drug-drug interactions: Digoxin; other Antiarrhythmics

Question 47

Targets for Cholesterol

Answer 47

\<5.0 mmol/L Total Cholesterol \<4.0 mmol/L Non-HDL \<2.0 mmol/L LDL 40% reduction of Non-HDL at 3 months

Question 48

Spironolactone

Answer 48

Drug class: Mineralocorticoid Receptor Antagonist (Aldosterone) Common indications: Hypertension; Primary Hyperaldosteronism; Severe Heart Failure; Hypokalaemia Other Important Drugs in Class: N/A Mechanism of action: Blocks action of Aldosterone at nephron, preventing upregulation of Na/K ATPase. This prevents sodium reabsorption and potassium secretion, increasing sodium and water loss. Important adverse drug reactions: Hyperkalaemia; Gynaecomastia; Impotence (males) Contraindications: Hyperkalaemia; Addison's Disease/Crisis Important drug-drug interactions: Potassium increasing drugs; pregnancy

Question 49

Sulfasalzine

Answer 49

Drug class: DMARD Common indications: RA; Infection Other Important Drugs in Class: Mesalazine Mechanism of action: Conjugate of 5ASA and sulfapyridine. 5ASA inhibits T-cell proliferation and neutrophil degranulation.Sulfa group fights infection Important adverse drug reactions: Myelosuppression; hepatitis Contraindications: N/A Important drug-drug interactions: N/A

Question 50

Nabilone

Answer 50

Drug class: Cannabinoid Common indications: Antiemesis (Chemotherapy) Other Important Drugs in Class: N/A Mechanism of action: Inhibits CTZ Important adverse drug reactions: Dizziness; Drowsiness Contraindications: N/A Important drug-drug interactions: N/A

Question 51

Alirocumab

Answer 51

Drug class: PCSK9 Inhibitor Common indications: Hypercholesterolaemia Other Important Drugs in Class: Evolocumab (Inclisiran) Mechanism of action: Inhibits PCSK9, preventing LDLR degredation Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions:N/A

Question 52

Beclometasone

Answer 52

Drug class: Inhaled Corticosteroid Common indications: Asthma; Allergic Rhinitis; COPD Other Important Drugs in Class: Fluticasone; Budesonide Mechanism of action: Prevent production of IL-1 and IL-6, reducing mucosal inflammation. ↑ß2 expression Important adverse drug reactions: local immunosuppressive action (candidiasis, hoarse voice) Contraindications: Pneumonia risk in COPD Important drug-drug interactions: N/A at normal doses

Question 53

Dalteparin

Answer 53

Drug class: Low Molecular Weight Heparin Common indications: DVT; PE Other Important Drugs in Class: Enoxaparin Mechanism of action: Potentiates ATIII, inhibiting Xa and IIa Important adverse drug reactions: Bleeding; Thrombocytopenia Contraindications: N/A Important drug-drug interactions: Anticoagulants

Question 54

Mycophenolate Mofetil

Answer 54

Drug class: Purine Analogue Common indications: Trnasplantation; SLE; Vasculitis Other Important Drugs in Class: N/A Mechanism of action: Inhibition of DNA replication in T and B cells Important adverse drug reactions: NVD; Infection; Myelosuppression Contraindications: N/A Important drug-drug interactions: N/A

Question 55

Hyoscine Hydrobromide

Answer 55

Drug class: M1R Antagonist Common indications: Antiemesis (motion sickness, bowel obstruction, those who can't take tablets) Other Important Drugs in Class: N/A Mechanism of action: Inhibits Vestibular Nuclei and CTZ Important adverse drug reactions: Sedation; Memory problems; Glaucoma; Dry mouth; Constipation Contraindications: N/A Important drug-drug interactions: N/A

Question 56

Bisacodyl

Answer 56

Drug class: Stimulant Laxative Common indications: Constipation Other Important Drugs in Class: Senna; Docusate Sodium Mechanism of action: Increase intestinal motility Important adverse drug reactions: Cramping; Nausea Contraindications: N/A Important drug-drug interactions: N/A

Question 57

Salmeterol

Answer 57

Drug class: Long Acting ß2 Agonist (LSABA) Common indications: Add on therapy in Asthma; prevents nocturnal and exercise induced attacks Other Important Drugs in Class: Formoterol (LFABA) Mechanism of action: Agnosies ß2R Important adverse drug reactions: Adrenergic - tachycardia, palpitations, anxiety, tremor, ↑glycogenolysis, ↑renin Contraindications: Should only be prescribed alongside ICS (can mask airway inflammation alone) Important drug-drug interactions: ß-Blockers

Question 58

Sodium Valproate

Answer 58

Drug class: GABA potentiator Common indications: Seizures; Manic phase of bipolar Other Important Drugs in Class: N/A Mechanism of action: Increases GABA synthesis and prevents GABA degradation - decreasing nerve firing Important adverse drug reactions: NV; Dizziness; Sedation Contraindications: Pregnancy (Spina bifida, impaired cognitive development) Important drug-drug interactions: CYP2C9 inhibitor

Question 59

Medroxyprogesterone Acetate

Answer 59

Drug class: Progesterone agonist Common indications: HRT; Contraceptive Other Important Drugs in Class: Hydroxyprogesterone Mechanism of action: Decreases endometrial hyperplasia in pts recieving oestrogen (HRT); Prevents contraception by altering cervical mucus and creating hostile endometrium Important adverse drug reactions: Amenorrhoea; Breakthrough bleeding; Dysmenorrhoea Contraindications: N/A Important drug-drug interactions: N/A

Question 60

Inclisiran

Answer 60

Drug class: PCKS9 Inhibitor Common indications: Hypercholesterolaemia Other Important Drugs in Class: (Alirocumab, Evolocumab) Mechanism of action: siRNA that inhibits translation of PCSK9 Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions: N/A

Question 61

Pyridostigmine

Answer 61

Drug class: Cholinesterase Inhibitor Common indications: myasthenia Gravis; Reversal of nondepolarising neuromuscular blockers Other Important Drugs in Class: Neostigmine Mechanism of action: Preventing of Acetylcholine degradation at NMJ Important adverse drug reactions: SSLUDGE Contraindications: N/A Important drug-drug interactions: Atropine

Question 62

Ciclosporin

Answer 62

Drug class: Calcineurin Inhibitor Common indications: Transplantation; Atopic Dermatitis; Psoriasis Other Important Drugs in Class: Tacrolimus Mechanism of action: Preventing IL-2 production Important adverse drug reactions: Infection; Eye Inflammation; Renal Toxicity Contraindications: Renal Impairment Important drug-drug interactions: CYP3A4 metabolised

Question 63

Salbutamol

Answer 63

Drug class: Short Acting ß2 Agonist Common indications: Symptom relief in Asthma and COPD; Prevention of bronchospasm prior to exercise Other Important Drugs in Class: Terbutaline Mechanism of action: Agnoises ß2R, reversing bronchoconstriction Important adverse drug reactions: Adrenergic - tachycardia, palpitations, anxiety, tremor, ↑glycogenolysis, ↑renin Contraindications: N/A Important drug-drug interactions: ß-Blockers; other adrenergic drugs

Question 64

Treatment Plan for Heart Failure

Answer 64

HFpEF - Manage Co-morbidities, Cardiac Rehabilitation programme HFrEF - ACEi/ARB and ßB (+ MRA if needed), Cardiac Rehabilitation programme

Question 65

Naloxone

Answer 65

Drug class: Opiod Antagonist Common indications: Opiod Overdose Other Important Drugs in Class: N/A Mechanism of action: Antagonises µR Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions: N/A

Question 66

Exenatide

Answer 66

Drug class: GLP-1R Agonist/Incretin Mimetics Common indications: T2DM Other Important Drugs in Class: Liraglutide Mechanism of action: Activate GLP-1R and resistant to degradation by DPP-4. ↑insulin secretion, ↓glucagon secretion, ↓gluconeogenesis, ↑satiety and ↓gastric emptying Important adverse drug reactions: GI upset; Decreased appetite; WEIGHT LOSS Contraindications: Renal Failure Important drug-drug interactions: Antidiabetics

Question 67

Lamotrigine

Answer 67

Drug class: Sodium Channel Blocker Common indications: Seizures Other Important Drugs in Class: Movicol Mechanism of action: Block sodium and glutamate Important adverse drug reactions: Ataxia; Dizziness; Photosensitivity Contraindications: N/A Important drug-drug interactions: CYP2C9

Question 68

Clopidogrel

Answer 68

Drug class: ADP Receptor Antagonist Common indications: Prophylaxis of Stroke, MI, Peripheral Vascular Disease Other Important Drugs in Class: Ticagrelor (reversible, already active; rapid); Prasugrel (activated by liver; rapid) Mechanism of action: Irreversibly inhibits binding of ADP to P2Y12 receptor - prevents activation of GPIIb/IIIa, preventing platelet aggregation. Activated by liver and slow working Important adverse drug reactions: Bleeding; GI Upset; Thrombocytopenia Contraindications: High bleed risk patients; Renal or Hepatic Impairment Important drug-drug interactions: Requires CYP Activation (inhibited by Ciprofloxacin, Omeprazole, Erythromycin, some SSRIs, other PPIs); other antiplatelets or anticoagulants

Question 69

Atropine

Answer 69

Drug class: Class V Antiarrhythmic/mAChR inhibitor Common indications: Bradycardia; AV block; Irritable Bowel; Anticholinesterase poisoning; Ocular inflammation Other Important Drugs in Class: Ipratropium; oxybutynin; solifenacin Mechanism of action: Blocks mAChR Important adverse drug reactions: Tachycardia; Mydriasis; delirium Contraindications: N/A Important drug-drug interactions: delays gastric emptying; additive anticholinergic effects with antihistamines and tricyclics

Question 70

Dabigatran

Answer 70

Drug class: IIa DOAC Common indications: VTE Other Important Drugs in Class: N/A Mechanism of action: Inhibitor of IIa Important adverse drug reactions: Bleeding Contraindications: N/A Important drug-drug interactions: CYP3A4

Question 71

Doxazosin

Answer 71

Drug class: α1-Adrenoreceptor Blocker Common indications: DPH; Hypertension Other Important Drugs in Class: N/A Mechanism of action: Block NAd at α1, decreasing peripheral resistance Important adverse drug reactions: Postural Hypotension; Dizziness; Syncope; Headache; Fatigue Contraindications: Postural Hypotension Important drug-drug interactions: Dihydropyridine CCB (↑ risk of Oedema)

Question 72

Paracetamol

Answer 72

Drug class: Analgesic and Antipyretic Common indications: Pyrexia; Pain Other Important Drugs in Class: N/A Mechanism of action: Inhibition of COX-2 in CNS; not known Important adverse drug reactions: Can cause hepatic failure in overdose Contraindications: Chronic Alcohol Use (W) Important drug-drug interactions: Additive renal toxicity with salicylates and NSAIDs

Question 73

Amlodipine

Answer 73

Drug class: Dihydropyridine type Calcium Channel Blockers Common indications: Hypertension Other Important Drugs in Class: Nifedipine; Nimodipine Mechanism of action: Blocks CCBs in Vascular Smooth Muscle, preventing Vasoconstriction Important adverse drug reactions: Hypotension; Ankle Oedema; Flushing; Headaches; Palpitations (compensatory tachycardia) Contraindications: Unstable Angina; Severe Aortic Stenosis Important drug-drug interactions: Simvastatin (amlodipine weakly inhibits CYP3A4, increases [statin])

Question 74

Metoclopramide

Answer 74

Drug class: D2R Antagonist Common indications: Antiemesis (GORD, Ileus, Motion Sickness, VErtigo, Chemotherapy, Palliation) Other Important Drugs in Class: Domperidone; Chlorpromazine; Haloperidol Mechanism of action: Increases ACh; Promotes gastric emptying; Increases peristalsis; Act on CTZ Important adverse drug reactions: Galactorrhoea; Extra-pyramidal effects; (Domperidone - sudden cardiac death) Contraindications: N/A Important drug-drug interactions: N/A

Question 75

Paclitaxel

Answer 75

Drug class: Mitotic Inhibitor Common indications: Cancer Other Important Drugs in Class: N/A Mechanism of action: Prevents depolymerisation of microtubles of spindle Important adverse drug reactions: NVD; alopecia; Myelosuppression; Peripheral Neuropathy Contraindications: N/A Important drug-drug interactions: N/A

Question 76

Methotrexate

Answer 76

Drug class: Folate Reductase Inhibitor Common indications: Leukaemias; Solid cancers; Psoriasis; Crohns; RA Other Important Drugs in Class: N/A Mechanism of action: Inhibits dihydrofolate reductase; prevents DNA replication. In non-malignant disease - not known Important adverse drug reactions: Mucositis; Myelosuppression; Hepatitis; Infection Contraindications: Pregnancy (Teratogen and Abortifacient) Important drug-drug interactions: Other myelosuppressives; V. highly protein bound - sulfonylureas, NSAIDs, Warfarin

Question 77

Cisplatin

Answer 77

Drug class: Reactive Platinum Compound Common indications: Cancer Other Important Drugs in Class: N/A Mechanism of action: Cross-links DNA strands Important adverse drug reactions: NV; Renal toxicity; ototoxicity and Tinnitus; Anaemia Contraindications: N/A Important drug-drug interactions: N/A

Question 78

Dipyridamole

Answer 78

Drug class: Phosphodiesterase inhibitor/A2R inhibitor Common indications: Secondary prophylaxis of Stroke and TIA Other Important Drugs in Class: N/A Mechanism of action: Inhibits A2R, preventing platelet aggregation. Inhibits phosphodiesterase, preventing cAMP degradation -\> inhibiting expression of GPIIb/IIIa Important adverse drug reactions: V+D; Dizziness Contraindications: N/A Important drug-drug interactions: Other antiplatelets and anticoagulants; Adenosine

Question 79

Ezetimibe

Answer 79

Drug class: Choleterol Absorption Inhibitors Common indications: Hypercholesterolaemia (adjunt to statin) Other Important Drugs in Class: N/A Mechanism of action: Inhibits NPC1L1, reducing Cholesterol Absorption Important adverse drug reactions: Abdo Pain; GI Upset; Angioedema Contraindications: Hepatic Failure Important drug-drug interactions: Statin (slightly increased risk of rhabdomyolysis); Ciclosporin

Question 80

Abciximab

Answer 80

Drug class: GPIIb/IIIa inhibitor Common indications: Prophylaxis of TE Other Important Drugs in Class: N/A Mechanism of action: Prevents fibrinogen and vWF binding to GPIIb/IIIa Important adverse drug reactions: Bleeding Contraindications: N/A Important drug-drug interactions: other antiplatelets and anticoagulants

Question 81

Gaviscon

Answer 81

Drug class: Alginate + Antacid Common indications: Dyspepsia Other Important Drugs in Class: N/A Mechanism of action: Sodium Alginate - forms film preventing reflux. AlOH/MgCO3 - buffers acid Important adverse drug reactions: Mg salts causes diarrhoea and Al salts cause constipation Contraindications: Na and K containing preparations can worsen renal failure; High sucrose in some - T2DM Important drug-drug interactions: Can reduce absorption of many drugs; Increases in urine alkalinity increases aspirin excretion

Question 82

Unfractionated Heparin

Answer 82

Drug class: Heparin Anticoagulant Common indications: VTE; PE; AFw/E Other Important Drugs in Class: N/A Mechanism of action: Bind to Antithrombin III, causing destruction of IIa and Xa - PARENTERAL Important adverse drug reactions: Bleeding; Thrombocytopenia Contraindications: N/A Important drug-drug interactions: other Anticoagulants

Question 83

Verapamil

Answer 83

Drug class: Non-Dihydropyridine Calcium Channel Blocker (Phenylalkylamine)/ Class IV Antiarrhythmic Common indications: Hypertension; Angina; SVT; Prevention of Migrane Headache Other Important Drugs in Class: N/A Mechanism of action: Blocks Calcium entry in Heart Tissue, decreasing Phase 2; and preventing Phase 0 in the SAN and AVN Important adverse drug reactions: Constipation; Bradycardia; Heart Block; Heart Failure Contraindications: Poor LV Function; AV Nodal Conduction Delay Important drug-drug interactions: ß-Blockers; Other Hypotensives; Other Antiarrhythmics

Question 84

Azathioprine

Answer 84

Drug class: Purine analogue Common indications: SLE + Vasculitis maintenance therapy; IBD; (6-MP - Leukaemia, Lymphoma) Other Important Drugs in Class: N/A Mechanism of action: Inhibits purine biosynthesis; blocks S phase. Metabolised by TPMT - highly polymorphic gene, so test TPMT first Important adverse drug reactions: Myelosuppression; Risk of malignancy; Infection; Hepatitis - test LFT Contraindications: Low TPMT Important drug-drug interactions: Allopurinol inhibits degradation

Question 85

Indapamide

Answer 85

Drug class: Thiazide-like Diuretic Common indications: Hypertension Other Important Drugs in Class: Bendroflumethiazide Mechanism of action: Inhibits Na/Cl Symporter - decreases Na and H2O reabsorption. ?reduces sensitivity to vasoconstrictors Important adverse drug reactions: Hypokalaemia; Hyponatraemia; Hyperuricaemia; Arrhythmia; Hyperglycaemia; Hypercholesterolaemia; Hyperlipidaemia Contraindications: Hypokalaemia; Hyponatraemia; Gout Important drug-drug interactions: NSAIDs; Potassium-lowering drugs

Question 86

Lidocaine

Answer 86

Drug class: Local Anaesthetic Common indications: Anaesthetic Other Important Drugs in Class: Bupivicaine; Procaine; Ropivicaine Mechanism of action: Blocks Na conduction Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions: N/A

Question 87

Diazepam

Answer 87

Drug class: Benzodiazapine Common indications: Anxiety; Status epilepticus; Alcohol withdrawal; Light Anasthaesia Other Important Drugs in Class: Lorazepam; Midazolam Mechanism of action: Activate GABAa, hyperpolarising neurones Important adverse drug reactions: Drowsiness; Dizziness' Lethargy; Cognitive and psychomotor impairment Contraindications: N/A Important drug-drug interactions: Additive effects with alcohol; CYP2C19 and CYP3A4

Question 88

Loperamide

Answer 88

Drug class: Opiod Agonist Common indications: Diarrhoea Other Important Drugs in Class: Codeine Mechanism of action: Activates µ-Opiod R - decreasing tone of smooth muscle and reduccing peristalsis Important adverse drug reactions: Constripation; Drowsiness Contraindications: Pregnancy Important drug-drug interactions: N/A

Question 89

Entacapone

Answer 89

Drug class: Catechol-O-methyl Transferase Inhibitor Common indications: Parkinsons Disease Other Important Drugs in Class: Opicapone Mechanism of action: Inhibits levodopa breakdown by COMT Important adverse drug reactions: Dyskinesia; NVD; Discoloured urine Contraindications: N/A Important drug-drug interactions: Erythromycin inhibits biliary excretion

Question 90

Vincristine

Answer 90

Drug class: Vinka Alkaloid Common indications: Cancer Other Important Drugs in Class: N/A Mechanism of action: Prevents assembly of microtubules and spindle Important adverse drug reactions: NV; Alopecia; Peripheral Neuropathy Contraindications: N/A Important drug-drug interactions: Decreases antibody response to live virus vaccines

Question 91

Prednisolone

Answer 91

Drug class: Corticosteroid Common indications: Inflammatory disease; Allergery; Asthma; Neoplasia; Autoimmunity; Antiemesis (perioperative, chemotherapy, palliation) Other Important Drugs in Class: Dexamethasone; Hydrocortisone; Betamethasone Mechanism of action: Prevent IL-1 and IL-6 production; Inhibit T-cell activation Important adverse drug reactions: Infection; Impaired wound healing; Adrenal suppression; Sarcopenia; Cushings Contraindications: Immunosuppression Important drug-drug interactions: Antiinflammatorys

Question 92

Atorvastatin

Answer 92

Drug class: Statin Common indications: Hypercholesterolaemia; Hyperlipidaemia Other Important Drugs in Class: Simvastatin Mechanism of action: HMG-CoA Reductase Inhibitor - reduces Cholesterol synthesis. This causes upregulation of LDLR Important adverse drug reactions: GI Disruption; Nausea; Headache; Myalgia; Rhabdomyolysis; Increased Liver Enzymes Contraindications: Renal or Hepatic Impairment; Pregnancy; Breastfeeding Important drug-drug interactions: CYP 3A4 (Amiodarone, Diltiazem, Macrolides); Amlodipine

Question 93

Carbidopa

Answer 93

Drug class: Decarboxylase Inhibitor Common indications: Parkinsons Disease Other Important Drugs in Class: Benserazide Mechanism of action: Inhbits degradation of levodopa Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions: N/A

Question 94

Ranitidine

Answer 94

Drug class: H2R Antagonist Common indications: Peptic Ulcer DIsease; GORD; Dyspepsia Other Important Drugs in Class: N/A Mechanism of action: Antagonises H2 receptors, preventing action of Histamine to increase local acid secretion Important adverse drug reactions: Diarrhoea; Headache Contraindications: Renal Impairment Important drug-drug interactions: N/A

Question 95

Carbamazepine

Answer 95

Drug class: Neuronal Na Blocker Common indications: Partial and Tonic-Clonic Seizures; Trigeminal Neuralgia; Bipolar Disorder Other Important Drugs in Class: N/A Mechanism of action: Block Na channels, decreasing firing Important adverse drug reactions: Ataxia; Drowsiness; Blurred Vision Contraindications: N/A Important drug-drug interactions: CYP3A4 inducer and substrate

Question 96

Ondasetron

Answer 96

Drug class: 5HT3R Antagonist Common indications: Antiemesis (everyone - often first line) Other Important Drugs in Class: Granisetron; Palonosetron Mechanism of action: Inhibits CTZ; Reduces GI motility and secretions Important adverse drug reactions: Constipation; Headache; Elevated LFTs; Long QT syndrome; Extra-pyramidal effects Contraindications: N/A Important drug-drug interactions: N/A

Question 97

Alendronic Acid

Answer 97

Drug class: Bisphosphonate Common indications: Osteoporosis; Paget's Other Important Drugs in Class: Pamidronate Disodium; Zoledronic Acid Mechanism of action: Prevents osteoclast precursors from attaching to bone; decreases metabolism of osteoclasts Important adverse drug reactions: N/A Contraindications: N/A Important drug-drug interactions: Absorption decreased by Ca2+, Antacids, Food and Drink (not water)

Question 98

Amiloride

Answer 98

Drug class: Potassium Sparing Diuretic Common indications: Prevention and Treatment of Hypokalaemia Other Important Drugs in Class: (Spironolactone) Mechanism of action: Blocks ENaC, preventing Sodium absorption (decreasing need for Na/K pump) Important adverse drug reactions: Hyperkalaemia; Arrhythmia Contraindications: Addison's; Potassium Supplements Important drug-drug interactions: Other K sparing drugs; ACEi; ARBs

Question 99

Phenytoin

Answer 99

Drug class: Na Blocker Common indications: Status Epilepticus; Seizures Other Important Drugs in Class: N/A Mechanism of action: Block sodium and glutamate Important adverse drug reactions: Ataxia; Diplopia; Nystagmus; Hirsutism Contraindications: N/A Important drug-drug interactions: Zero order kinetics; CYP3A4 inducer and CYP2C19 substrate

Question 100

Flecanaide

Answer 100

Drug class: Class I Antiarrhythmic Common indications: Supraventricular Tachycardias; PVCs; WPW syndrome Other Important Drugs in Class: Lidocaine Mechanism of action: Slows Phase 0; Decreases automaticity; Increases refractory period Important adverse drug reactions: Pro-arrhythmia; sudden death with chronic use; increased ventricular response to AFib or Flutter; CNS and GI effects Contraindications: Structural Heart Disease Important drug-drug interactions: N/A

Question 101

Adenosine

Answer 101

Drug class: Class V Antiarrhythmic/Adenodise Common indications: Termination of Re-entrant Supraventricular Tachycardia Other Important Drugs in Class: N/A Mechanism of action: Binds to A1R, blocking Adenylyl Cyclase -\> opens K+ channels causing hyperpolarisation in AVN and SAN Important adverse drug reactions: Transient Asystole (suppression of SAN) Contraindications: N/A Important drug-drug interactions: Dipyridamole (A2R inhibitor)

Question 102

Gliclazide

Answer 102

Drug class: Sulfonylureas Common indications: T2DM Mechanism of action: Closes Pancreatic ß-cell ATP-Sensitive K-channels, preventing K efflux and depolarising ß-cells. Causes influx of Ca, and insulin release. Important adverse drug reactions: Mild GI Upset; Hypoglycaemia; Weight Gain (action of insulin) Contraindications: Hepatic or Renal Impairment; Risk of Hypoglycaemia Important drug-drug interactions: Other hypoglycaemic agents; Loop and Thiazide-like Diuretics

Question 103

Fenofibrate

Answer 103

Drug class: Fibric Acid Derivative Common indications: Hyperlipidaemia; Hypercholesterolaemia Other Important Drugs in Class: N/A Mechanism of action: Activates PPARα (transcription factor that ↑LDLR + lipoprotein lipase) Important adverse drug reactions: Hyperlipidaemia; Hypercholesterolaemia Contraindications: Cholelithiasis; GI Upset; Myositis Important drug-drug interactions: Warfarin (increases anticoagulation)

Question 104

Aspirin

Answer 104

Drug class: COX-1 selective Non-Steroidal Anti-Inflammatory Drug Common indications: Prophylaxis of MI, TIA, and Stroke; Inflammatory Disorders; Pyrexia; Pain Other Important Drugs in Class: N/A Mechanism of action: Inhibition of prostaglandin synthesis (TXA2 and PGI2); prevents platelet aggregation and pro-inflammation Important adverse drug reactions: GI Irritation; GI Bleeding; Haemorrhage; Hypersensitivity Contraindications: Reye's Syndrome (avoid \<16yrs); Hypersensitivity; 3rd Trimester (closes DA) Important drug-drug interactions: other antiplatelets and anticoagulants

Question 105

CYP Inducers and Inhibitors

Answer 105

Inducers - CRAP GPs Carbamazepines Rifampicin Alcohol Phenytoin Griseofulvin Phenobarbitone Sulfonylureas Inhibitors - SICKFACES.COM Sodium Valproate Isoniazid Cimetidine Ketoconazole Fluconazole Alcohol and Grapefruit Juice Chloramphenicol Erythromycin Sulfonamides Cirpofloxacin Omeprazole Metronidazole

Question 106

Protein Bound Drugs

Answer 106

NSAIDs - displace the rest Methotrexate Sulfonylureas Warfarin