Hyms Lecture-Only Pharmacology

Front 1

Bendroflumethiazide

Back 1

Thiazide diuretics. Blocks Na+ reabsorption → ↓ H2O reabsorption → ↓total blood volume

↓BP

Front 2

Atenolol/Propranolol

Back 2

β-blockers. Antagonist of β-adrenergic receptors in heart + juxtaglomerular cells (secrete renin). Atenolol = β1, Propranolol = β1+2

↓ BP, ↓HR

Front 3

Doxazosin, Prazosin

Back 3

α adrenoreceptor blocker of smooth muscle @ precapillary sphincter. SE: 1st dose hypotension

↓ BP

Front 4

Amlodipine

Back 4

Ca2+ antagonists. Inhibit Ca2+ influx in smooth muscle → vasodilation

↓BP

Front 5

Captopril

Back 5

ACE inhibitors. ↓ Angiotensin II, by blocking Ang I→Ang II

↓BP

Front 6

Losartan

Back 6

Angiotensin receptor blockers. Block Angiotensin II binding to AT1 receptor.

↓BP

Front 7

spironolactone

Back 7

Aldosterone receptor blocker, ↓renal absorption of Na+ → ↓H2O reabsorption ↓total blood volume

↓BP

Front 8

Omeprazole

Back 8

PPI. Irreversibly inhibits H+/K+ ATPase pump.

Peptic ulcers

Front 9

Clarithromycin

Back 9

Macrolide antibiotic. Blocks RNA translation to peptides.

Antibiotic, Peptic ulcers (in combo with PPI)

Front 10

Amoxicillin

Back 10

Penicillins. Inhibits peptidoglycan, and thus bacterial cell wall formation

Antibiotic, Peptic ulcers (in combo with PPI)

Front 11

Metronidazole

Back 11

Binds to DNA + inhibits nucleic acid synthesis in anaerobic bacteria.

Antibiotic, Peptic ulcers (in combo with PPI)

Front 12

Ranitidine

Back 12

Histamine H2 antagonists.

Peptic ulcers

Front 13

Misoprostol

Back 13

Prostaglandin agonist.↓HCl secretion,↑mucous secretion

Peptic ulcers

Front 14

Hyoscine

Back 14

Muscarinic cholinergic antagonist. Acts in CTZ

Antiemetic

Front 15

Chlorpromazine, Perphenazine + Domperidone

Back 15

Azine antipsychotics Dopamine receptor (D2) antagonist. Acts in CTZ.

Antiemetic

Front 16

Metclopramide

Back 16

D2 antagonist + mixed 5HT3/4 antagonist. Acts in CTZ

Antiemetic

Front 17

Ondansetron

Back 17

5HT antagonist, ↓ vagal activity, acts in CTZ.

Antiemetic

Front 18

Cyclizine, cinarizine, promethazine

Back 18

Histamine H1 antagonists. Act in CTZ.

Antiemetic

Front 19

Olanzapine + Risperidone (2nd Gen), Haloperidol (1st gen)

Back 19

Antipsychotic D2 receptor antagonists. H1, muscarinic, α-adreno + 5-HT receptor antagonists → SIDE EFFECTS, as well as extrapyramidal SEs due to DA blockage.

Schizophrenia

Front 20

Amytriptyline, Lofepramine

Back 20

Tricyclic antidepressants. Block NA + 5-HT reuptake transporters. SEs as antipsychotics (except no DA extrapyramidal)

Depression

Front 21

Fluoxetine, Citalopram

Back 21

SSRIs. Block 5-HT reuptake transporter (SERT). SEs: nausea, vomiting, dependancy, sexual dysfunction, ↑ suicidal ideation, BUT safer in overdose c.f. tricyclics.

Depression + Anxiety

Front 22

Phenelzine, Medobemide

Back 22

MAO inhibitors. SEs: hypertensive crisis if diet rich in Tyramine (cheese + bovril)

Depression + Anxiety

Front 23

Lithium Carbonate (Priadel/Camcolit)

Back 23

↓DA+Glu (excitatory), ↑GABA (inhibitory). Affects 2nd messengers in intracellular signalling cascade. Narrow therapeutic window.

Bipolar Disorder

Front 24

Diazepam, Lorazepam, Temazepam

Back 24

Benzodiazepines. Bind to GABA receptor and potentiate it's effect. SEs: Drowsiness(hypnotic), dependance, resp. depression with alcohol.

Anxiety, Muscle spasms, hypnotic

Front 25

Digoxin/Digitalis

Back 25

Inhibits N+/K+ ATPase, ↑ Na+, Na+/Ca2+ exchanger used, ↑ Ca2+, +ve inotropy, -ve chronotropy

↓HR

Front 26

Ezitimibe

Back 26

blocks gut absorption of cholesterol, used in combo with statins

↓Cholesterol

Front 27

Atorvastatin

Back 27

Statins. Inhibits HMG CoA reductase, ↓de novo Cholesterol

↓Cholesterol

Front 28

Cholestyramine

Back 28

Binds to bile acids + ↑excretion, therefore liver uses cholesterol to make more.

↓Cholesterol

Front 29

Bezafibrate, Clofibrate

Back 29

↑HDL ↓TAG

↓Cholesterol

Front 30

Nicotinic acid

Back 30

High doses↑HDL ↓VLDL, LDL

↓Cholesterol

Front 31

Na Valproate

Back 31

Blocks Na ion channels weakly + ↑ opening time of GABA

epilepsy, anxiety, bipolar, PTSD

Front 32

Donepezil

Back 32

Acetylcholinesterase antagonist

Alzheimer's

Front 33

Ketamine

Back 33

Antagonist of NMDA receptor, involved in Glu neurotransmission

Anaesthesia, Analgesic, Crazy horses

Front 34

Metformin

Back 34

Biguanide. Activates AMP kinase + improves insulin resistance: ↑skeletal muscle glucose uptake ↓glucose absorption from intestine ↓ glycogenolysis + gluconeogenesis(liver). Weight neutral. SE ↓B12

TII Diabetes

Front 35

Gliclazide, Glimepiride

Back 35

Sulphonylureas. Stimulate insulin secretion by closing ATP-sensitive K+ channels on β-cells. SE weight gain, hypoglycaemia

TII Diabetes

Front 36

Troglitazone, Rosiglitazone, Pioglitazone

Back 36

Thiazolidinediones/glitazones. PPARγ agonist, acts as insulin sensitiser in liver,adipose +skeletal muscle. SE weight gain, oedema, bonefracture.

TII Diabetes

Front 37

Exenatide, Liraglutide

Back 37

GLP-1 agonists. ↑ insulin release + ↓ glucagon release, ↓ speed of gastric emptying (carbs absorbed more slowly), SE: ↓ apetite → weight loss, GIT problems, pancreatitis?

TII Diabetes

Front 38

Sitagliptin, Vildagliptin, Saxagliptin, Linagliptin

Back 38

DPP-4 inhibitors. Block degredation of GLP-1. Weight neutral. Linagliptin secreted in bile, useful for pts with renal failure. SE acute pancreatitis, GIT problems, dermatitis, resp. infxns

TII Diabetes

Front 39

Dapaglifozin, Canaglifozin

Back 39

SGLT-2 inhibitors. Inihibits SGLT-2 in proximal convoluted tubule → ↓glucose reabsorption. No risk of hypo. SE weight loss, ↑GU infxns

TII Diabetes

Front 40

Insulin

Back 40

Various preparations: short (humulin S), intermediate (humulin 1/Neutral protamine) + long-acting. Premixed = combo of short+intermediate.

TI + TII diabetes

Front 41

Carbimazole, Propylthiouracil

Back 41

Thionamides. Inhibit thyroid peroxidase (no I-→I). PTU also inhibits T3→T4.

Hyperthyroidism

Front 42

Radioactive I

Back 42

Death of thyroid cells. Given if drugs unsuccessful/pt is older. SE: iatrogenic hypothyroidism

Hyperthyroidism

Front 43

Viagra(sidenafil)

Back 43

Inhibits phosphodiesterase-5, ceasing cGMP hydrolysis

Erectile Dysfunction

Front 44

Biglutamide

Back 44

Androgen receptor antagonist

Prostate Cancer

Front 45

Finasteride

Back 45

reductase inhibitor (blocks testeosterone→ dihydrotestosterone

Prostate Cancer

Front 46

Desogestrel, Etonogestrel, Levonorgestrel

Back 46

Progesterone nuclear hormone receptor agonists.Inhibits LH (no LH surge, no ovulation). Thicken mucus, prevent ovulation, causes endometrial atrophy (the holy trinity)

SE: VTE, Menstrual irregularities

Contraception

Front 47

Estradiol sulphate/valerate, Estriol

Back 47

Oestrogen nuclear hormone receptor agonists. Inhibit FSH, preventing follicle maturation. Thicken mucus, prevent ovulation, causes endometrial atrophy (the holy trinity)

SE: VTE

Contraception

Front 48

Orlistat

Back 48

Pancreatic lipase inhibitor

Obesity

Front 49

Hemicholinium

Back 49

Blocks presynaptic reuptake of choline by high affinity transporter. Indirect antagonist acetylcholine antagonist.

Causes gradual paralysis. Not clinically used

Front 50

Botulinum

Back 50

Blocks release of Ach-containing vesicles

Cosmetic

Front 51

Edrophonium, Neostigmine, Physiostigmine, Pyridostigmine

Back 51

Competetive acetylcholinesterase inhibitors.

Myasthenia Gravis, Anaesthesia

Front 52

Sarin

Back 52

Irrevesible anticholinesterase. Antidote = Pralidoxime (cleaves sarin-cholinesterase bonding)

Nerve Gas

Front 53

Curare, Tubocurarine, Atracurium, Pancuronium, Mivacurium

Back 53

Nicotinic cholinergic antagonists

Muscle relaxants

Front 54

Suxamethonium

Back 54

Nicotinic agonist. Causes temporary paralysis by depolarising neuron, followed by muscle relaxation. V SHORT period of effect <1min

Muscle relaxant

Front 55

Atropine, Hyoscine (seeB3), Tropicamide

Back 55

Muscarinic antagonist.

Dilates pupils (ATROPINE)

Front 56

Pilocarpine

Back 56

Muscarinic agonist.

Glycoma

Front 57

Cocaine

Back 57

Na+ channel blocker

Drug of abuse

Front 58

Salbutamol, Salmaterol

Back 58

β2 adrenoreceptor agonists → bronchodilator

Asthma

Front 59

Isoprenaline, adrenaline, noradrenaline

Back 59

β1+2 adrenoreceptor agonists (NA = β1 only)

Asthma + heart block (ISOPRENALINE)

Front 60

Phenoxybenzamine

Back 60

Non-selective α-adrenoreceptor antagonist

↓BP + Anaesthetic

Front 61

Alendronate, Resindronate, Etindronate

Back 61

Biphosphonates. Inhibits osteoclastic activity

Osteoporosis

Front 62

Calciferol

Back 62

Vitamin D agonist

Osteoporosis, Vit. D deficiency

Front 63

Aspirin, Indomethacin, Ibuprofen, Diclofenac

Back 63

NSAIDs. COX1+2 inhibitors. Ibuprofen reversible inhibitor. SE: Gastric ulcers, bleeding.

Anti-inflammatory

Front 64

Paracetamol

Back 64

COX inhibition but not NSAID.

Analgesic

Front 65

Celecoxib, Etoricoxib

Back 65

Selective COX-2 inhibitors

Anti-inflammatory

Front 66

Hydrocortisone, Prednisone, Prednisolone, Dexamethasone, Betamethasone

Back 66

Glucocorticoids. Bind to cytoplasmic receptor, Hsp90 released, steroid-receptor complex enter cell and binds nuclear receptor to influence transcription. ↓ COX. Iipocortin produced(inhibits lipoxygenase production of leukotrienes) SE: Osteoporosis, immunodeficiency

Anti-inflammatory

Front 67

Chlorphenamine, Promethazine, Cetirizine, fexofenadine

Back 67

Antihistamines. H1/H2 antagonists. SE: Sedation (Chlorphenamine, Promethazine)

Anti-inflammatory

Front 68

Cyclosporine A

Back 68

Binds to cyclophilin protein (CpN) + inhibits calcineurin, which is key for IL-2 gene expression.

Anti-inflammatory

Front 69

Tacrolimus

Back 69

Binds to FK binding protein. Inhibits calcineurin (as Cyclosporine A)

Anti-inflammatory

Front 70

Rapamycin

Back 70

Binds FK binding protein and inhibits mTOR (molecular target of rapamycin)

Anti-inflammatory

Front 71

Morphine, Diamorphine, Codeine, Tramadol

Back 71

Opioids. CNS opioid receptor agonists.

Analgesics