Pharmacology - Drug List

Front 1

Cimetidine (Magicul)

Back 1

H2 Receptor Antagonist (Peptic Ulcers)
Reduces gastric (acid/pepsin) secretion by blocking H2 receptors.
Crosses BBB - CNS depression/excitation
Inhibits CYP450

Front 2

Ranitidine (Zantac, Rani 2)

Back 2

H2 Receptor Antagonist (Peptic Ulcers)
Similar to cimetidine, but more potent and fewer ADR (cannot cross BBB), fewer interactions

Front 3

Omeprazole (Omepral, Losec, Acimax)

Back 3

Proton Pump Inhibitor (Peptic Ulcers)
Irreversibly inhibits H+/K+-ATPase (proton pump) in parietal cells
Prodrug, activated by acidity of parietal cells

Front 4

Misoprostol (Cyotec)

Back 4

Prostaglandin E1 Analogue (Peptic Ulcers)
Suppresses acid secretion + increases bicarbonate and mucus secretion
ADR: diarrhoea, abdominal pain

Front 5

Bismuth Chelate

Back 5

Toxic to H. Pylori (Peptic Ulcers)
Coats Ulcer base, adsorbs pepsin
Enhances PG + bicarbonate secretion

Front 6

Antacids (Mylanta, Gaviscon)

Back 6

Neutralise stomach acids
ADRs: acid/base + electrolyte disturbances
Interacts with cimetidine/ranitidine

Front 7

Metoclopramide (Maxolon) & Domperidone (Motilium)

Back 7

Dopamine receptor antagonist (Anti-emetic)
also faciliates gastric emptying + intestinal activity (less food left to vomit)
Domperidone does not cross BBB (so still works on Chemical Trigger Zone)

Front 8

Types of Laxatives

Back 8

Osmotic - lactulose
Bulk forming - bran
Lubricant - liquid paraffin
Stimulant Purgatives - bisacodyl, senna
Parasympathomimetics - bethanecol

Front 9

Antidiarrhoeal drugs

Back 9

Bulk forming laxatives
Antimotility drugs - opioids, antimuscarinics
Antispasmodics - antimuscarinics (buscopan)

Front 10

Ulcerative Colitis + Crohn's Disease

Back 10

Glucocorticoids, sulfsalazine (anti-inflammatories?)
Immunosuppressants (azothioprine, mercaptopurine)

Front 11

Cholestyramine (Questran) + Colestipol (Colestid)

Back 11

Bile acid binding resins (hyperlipidaemia)
bind bile acids in intestinal lumen (prevent enterohepatic recycling)
decreases absorption of exogenous cholesterol
increases metabolism of endogenous cholesterol into bile acids
ADRs: nausea, bloating, constipation, diarrhoea, unpleasant taste

Front 12

Clofibrate, gemfibrozil (Gemhexal), fenofibrate (Lipidil), ciprofibrate + bezafibrate

Back 12

Fibrates (hyperlipidaemia)
agonists at PPAR-alpha
Stimulate lipoprotein lipase (break down lipids)
Reduces circulating VLDL and plasma LDL, increases plasma HDL
ADRs: myositis, GIT symptoms

Front 13

Fluvastatin (Vastin), Pravastatin (Pravachol, Lipostat), Atorvastatin (Lipitor), Simvastatin (Zocor, Lipex), Lovastatin

Back 13

Statins (Hyperlipidaemia)
Inhibit HMG-CoA Reductase (rate-limiting step in cholesterol synthesis)
decreases cholesterol synthesis
increases synthesis of LDL receptors (+ rate of removal of LDL from plasma)
ADRs: myositis

Front 14

Nicotinic acid

Back 14

(Hyperlipidaemia)
Inhibits VLDL production
Activates lipoprotein lipase (break down lipids)
ADRs: flushing, gout, palpitations

Front 15

Probucol

Back 15

(Hyperlipidaemia)
Lowers plasma HDL + LDL
Inhibits atherogenesis (antioxidant action reducing LDL oxidation + foam cell formation)
ADRs: GIT effects, ventricular tachycardia

Front 16

Fluoxetine (Prozac), Buspirone (Buspar), Sumatriptan (Imigran), ergot alkaloids, Tegaserod (Zelmac)

Back 16

Serotonin Agonists
Fluoxetine (SSRI) - depression + other indications
Buspirone - anxiety
Sumatriptan - migraine
Ergot alkaloids - migraine
Tegaserod - constipation dominant IBS (increase gastric motility)

Front 17

Methysergide (Deseril), Cyproheptadine (Periactin), Ketanserin, Clozapine (Clopine), Ondansetron (Zofran)

Back 17

Serotonin Antagonists
Methysergide+Cyproheptadine - carcinoid, migraine
Ketanserin - antihypertensive
Clozapine - schizophrenia
Ondansetron - chemotherapy-induced nausea/vomiting

Front 18

Sumatriptan (Imigran), Zolmitriptan (Zomig), Naratriptan (Naramig), Eletriptan

Back 18

Migraine Treatment
5HT 1B/D receptor agonists
Constrict large arteries, inhibit trigeminal nerve transmission (preventing dilation)
Taken at start of attack (once aura passes)
SE: coronary vasoconstriction

Front 19

Ergotamine (Cafergot)

Back 19

Migraine
5HT1 partial agonist, alpha-1 agonist
Administer prior to attack
SE: potential severe long-lasting vasoconstriction

Front 20

Methysergide (Deseril)

Back 20

Migraine Prophylaxis
5HT2 antagonist/partial agonist
Not effective in active migraine attack or preventing an impending attack
SE: nausea, vomiting, diarrhoea
Toxicity - 3-4week break every 6 months

Front 21

Propranolol (Deralin), Amitriptyline (Endep), Valproic acid (Valpro), NSAIDs

Back 21

Migraine Prophylaxis
Propanolol - most common for continous prophylaxis

Front 22

Carbamazepine (Tegretol)

Back 22

Anti-epileptic drug
V. effective - complex partial seizures + generalised tonic-clonic
Not effective in absence seizures
Blocks use/voltage-dependent Na+ channels
Induces own metabolism (CYP3A4)
SEs: drowsiness, dizziness, double vision, confusion
Start low doses + increase slowly

Front 23

Sodium Valproate (Valpro)

Back 23

Anti-epileptic drug
Effective against absence seizures and other generalised seizures (can use in children)
Block voltage activated Na+ channel, decr. T-type Ca2+ currents, increase GABA in brain
low toxicity/sedation
SEs: GI upset, nausea, vomiting, teratogenic (neural tube)

Front 24

Ethosuximide (Zarontin)

Back 24

Anti epileptic
1st choice against absence seizures
Inihibit T-type Ca2+ channels
May precipitate tonic-clonic
SEs: headache, lethargy, hiccup, euphoria

Front 25

Phenytoin (Dilantin)

Back 25

Anti-epileptic
For partial + generalised seizures
Worsens absence seizures
Blocks use-dependent Na+ conductance, decr. Ca2+ influx into cells
Induces 3A4, 2C9 - own metabolism can be saturated
Highly protein bound
SEs: double vision, ataxia, confusion

Front 26

Phenobarbitone

Back 26

Anti-epileptic
Still considered useful for infant seizures
Increases GABA-inhibition, decreases glutamate-excitation
SEs: sedation -> respiratory depression (due to excess GABA)

Front 27

Benzodiazepines - diazepam (Valium), lorazepam (Ativan)

Back 27

Anti-epileptic
Given IV for status epilepticus
Enhances GABA transmission
SEs: sedation, tolerance

Front 28

Vigabatrin (Sabril)

Back 28

Newer anti-epileptic
For partial seizures
Inhibits GABA transaminase (increasing GABA)
Short half-life, but irreversible inhibition
SEs: visual field defects

Front 29

Lamotrigine (Lamictal)

Back 29

Anti-epileptic
For partial + generalised seizures
Blocks Na+ channels
Useful for focal + absence seizures
Quite safe in pregnancy

Front 30

Topiramate (Topamax)

Back 30

Anti-epileptic
For partial seizures that lead to secondary generalised
Blocks Na+ channels, increase GABA, blocks AMPA glutamate receptors
Similar to phenytoin (but no saturation/induction)

Front 31

Gabapentin (Neurontin)

Back 31

Anti-epileptic
For partial seizures
GABA-analogue, altering its metabolism, non-synaptic release and transport
Relatively safe, few drug interactions

Front 32

L-dopa + benserazide (Madopar) or carbidopa (Sinemet, Kinson)

Back 32

Parkinson's Disease
Increases dopamine activity
L-dopa: immediate precursor of DA, can pass BBB
Combined with benserazide/carbidopa (dopa decarboxylase inhibitor)
SEs: anorexia, nausea, vomiting, mild hypotension, dyskinesias, confusion

Front 33

Cabergoline (Cabaser)

Back 33

Parkinson's Disease
Ergoline D2 Agonist
Can be first line or partial L-dopa replacement
SEs: nausea, sedation, orthostatic hypotension, heart valve problems

Front 34

Apomorphine (Apomine)

Back 34

Parkinson's Disease
Dopamine agonist for when other treatments fail
Start SC dosing in hospital, remove other PD medications
SEs: severe, highly emetogenic

Front 35

Ropinirole (Repreve)

Back 35

Parkinson's Disease
Non-ergoline Dopamine-2 agonist
Fewer SEs than other DA agonists
May be neuroprotective

Front 36

Selegiline (Selgene), Entacapone (Comtan), Amantadine (Symmetrel)

Back 36

Parkinson's Disease
Selegiline: MAO-B inhibitor (increases CNS DA), minor effect alone
Entacapone: COMT peripheral inhibitor, increases L-dopa plasma half-life
Amantadine: increase neuronal DA release, anticholinergic (reduce tremors), NMDA receptor antagonist

Front 37

Benztropine (Cogentin)

Back 37

Parkinson's Disease
ACh antagonist
Blocks ACh (excitatory) effects on neurons + presynaptic inhibitory effect on DA terminals
Improves tremor
Start with low dose, increase till benefits occur
SEs: anticholinergic (drowsiness, confusion, dry mouth, blurred vision)

Front 38

Neuroprotective agents against reactive oxygen species (Alzheimer's disease)

Back 38

NMDA antagonists - stroke
Riluzole (glutamate modulator) - ALS + HD
Coenzyme Q10 - PD

Front 39

Donepezil (Aricept)

Back 39

Alzheimer's disease
Cholinesterase Inhibitor
halflife: 70hrs
Metabolised by 2D6 + 3A4 (interacts w/ ketoconazole)
SEs: nausea, diarrhoea, vomiting, insomnia
CI: peptic ulcer, GI obstruction

Front 40

Rivastigmine (Exelon)

Back 40

Alzheimer's disease
AChE + BuChE (slowly reversible) - plasma t1/2: 1.5h, effect: 10hrs
More selective for CNS
Metabolism by esterases at synapse, not liver
Reduce dose in renal/hepatic impairment
SEs: as for donepezil (nausea, vomiting, diarrhoea, insomnia)

Front 41

Galantamine (Reminyl)

Back 41

Alzheimer's disease
AChEi + allosteric modulator of nicotinic ACh receptors
Short acting (t1/2 7-8h)
CYP2D6 + 3A4
Clearance decreases with age
CI: severe renal/hepatic impairment

Front 42

Possible future targets for Alzheimer's disease?

Back 42

Statins
NSAIDS
Inhibitors of amyloid beta protein formation and aggregation
- beta/gamma secretase inhibitors
- THC

Front 43

Riluzole (Rilutek)

Back 43

Huntington's disease
Inhibits Glu release
NMDA R antagonist

Front 44

Huntington's disease treatments

Back 44

Movement disorders
- riluzole + olanzapine
Depression
- SSRIs + mirtazapine
Psychosis and behavioural problems
- atypical antipsychotic drugs

Front 45

Buspirone (Buspar)

Back 45

Anxiolytic
Agonist at 5-HT1A (pre/post synaptic Rs)
Longterm: 5-HT1A downregulation, 5-HT release increase
High 1st pass, CYP3A4
SEs: dizziness, nausea, nervousness, headache
CI: MAOIs, alcohol, epilepsy (other CNS), renal/hepatic impairment
Less dependence than BZDs, better in naive subjects

Front 46

Lorazepam (Ativan), temazepam (Temaze), Zolpidem (Stilnox), Diazepam (Valium), Midazolam (Hypnovel), Clonazepam (Paxam)

Back 46

Benzodiazepines (Sedatives)
Bind to alpha1+2 subunits on GABA-R -> increase GABA, channel opening
Effects: sedation, muscle relaxant, anxiolytic, anticonvulsant
Crosses BBB
SEs: Safe alone, sedation, confusion, co-ordination, tolerance, dependance
Heightened risk in elderly (hip fractures)

Front 47

Zaleplon, zopiclone (Imovane), Zolpidem (Stilnox)

Back 47

New generation BZD Hypnotics
Bind to alpha1 subunit GABA-R (more selective)
Short acting, no metabolites (less daytime sedation)
Possibly less tolerance/dependence
Still problematic in elderly (falls)

Front 48

Flumazenil (Anexate)

Back 48

Benzodiazepine antagonist
Uses: BZ overdose, reverse anaesthesia
Administer IV
SEs: may precipitate anxiety, confusion, nausea
(conformational change in receptor, may act as inverse agonist)

Front 49

Phenobarbital, Thiopentone (Pentothal)

Back 49

Barbituates
Non-selective CNS depressants
- sedation -> death
Potent CYP450 inducers
Tolerance/dependence
Phenobarbital: anticonvulsant
Thiopentone: IV anaesthetic

Front 50

Chlorpromazine (Largactil), thiordazine (Aldazine), fluphenazine (Anatensol)

Back 50

Phenothiazines (Antipsychotic drugs)
DA-2 Receptor blocker
Low potency
SEs: sedation, neuroendocrine effects, seizures, extrapyramidal symptoms, anticholinergic.

Front 51

Clozapine (Clopine), olanzapine (Zyprexa)

Back 51

Atypical antipsychotic agents
Less D2, more D1, D4 block - also, 5HT, alpha 1, H and ACh
Less extrapyramidal effects (may cure tardive dyskinesia)
SEs: agranulocytosis (not for olanzapine), seizures, diabetes, weight gain

Front 52

Remoxipride, sulpiride, pimozide, risperidone (Risperdal)

Back 52

New antipsychotics
Sulpiride: selective D2 block, less extrapyramidal
Pimozide: long acting, 'dirty'
Risperidone: D2 + 5HT2 block, fewer extrapyramidal

Front 53

Lithium Bicarbonate (Lithicarb)

Back 53

Antimanic (mood stabiliser)
MOA: replaces sodium in excitable cells and depolarises membranes, reduces cAMP, interferes w/ PIP3 transduction pathway
Acute: only controls mania
Prophylactic: controls mania + depression
SEs: polyuria/dipsia (ADHi), thyroid enlargement, nausea, vomiting, tremor

Front 54

Moclobemide (Arima)

Back 54

For depression
MAOI (specifically MAO-A)
reversible
less interaction w/food (yeast extract etc.)

Front 55

Imipramine (Tofranil), Amitryptiline (Endep), Nortryptiline (Allegron)

Back 55

Tricyclic antidepressants
Inhibit NA and/or 5-HT reuptake, also block M + H receptors
2-4wk delay onset (downregulation of 5-HT2, beta-1+2 receptors?)
SEs: excitement, delirium, convulsions, atropine-like effects (reverse w/ physostigmine)

Front 56

Fluoxetine (Prozac), Paroxetine (Aropax), Sertraline (Zoloft), Citalopram (Cipramil), Escitalopram (Lexapro), Fluvoxamine (Luvox)

Back 56

Specific Serotonin Reuptake Inhibitors (SSRIs)
Selectively block serotonin reuptake pump, inhibit rate of firing of 5HT neurons, reduces release of 5HT
Long term: downreg of 5HT1A autoreceptors, post-syn 5HT-Rs + beta-1 Rs, disinhibition of 5HT release at axon terminals
SEs: 5HT3 - nausea, GIT, diarrhoea, headache
5HT2 - agitation, anxiety, insomnia
SSRI discontinuation syndrome

Front 57

Venlafaxine (Efexor), Nefazodone, Reboxetine (Edronax)

Back 57

Selective Noradrenaline Reuptake Inhibitors (SNRIs)
Venlafaxine: Inhibit 5HT, NA, DA uptake (like SSRI + TCA)
SEs: nausea, agitation, headache
Nefazodone: selective agonist of post-syn 5-HT2A receptors
SEs: somnolence, asthenia
Reboxetine: inhibits NA, 5HT (weakly) uptake, alpha-2 antagonist
SEs: low toxicity, dry mouth, urinary retention, sweating

Front 58

Bupropion (Zyban)

Back 58

Dopamine-Noradrenaline Reuptake Inhibitor (DNRI)
Weak antidepressant
Inhibits reuptake of DA + NA
Used as pharmacotherapy for cessation of smoking

Front 59

St. John's Wort

Back 59

Antidepressant (anxiety, anti-viral effects, wound healing)
Inhibit binding at AChM, 5-HT + NA sites, melatonin secretion, increased DA turnover
Clinical trials: as effective as TCAs in depression (w/ less SEs)
Drug interactions (warfarin + others)
Serotonin syndrome

Front 60

Amphetamine, dexamphetamine, methamphetamine, methylphenidate, fenfluramine

Back 60

Psychomotor Stimulants
L-amphetamine (periphery), D-amphetamine (centrally)
Act to displace cytosolic DA, may also release NA and 5-HT
Weakly blocks uptake-1 and MAO (so TCA + MAOi potentiate effect)
Cause: euphoria, confidence, improved mental/physical performance, appetite suppression
Uses: ADHD, narcolepsy

Front 61

Modafinil, atomoxetine

Back 61

Psychomotor stimulants
Modafanil: unknown MOA
Atomoxetine: selective for presynaptic NA transporter, 5-HT, DA (weakly), minimal for other NA transporters, 5-HT2 and GABA-A (moderate)
Uses: modafinil - narcolepsy, severe chronic shift work disorder, obstructive sleep apnoea
atomoxetine - ADHD

Front 62

Cocaine

Back 62

Psychomotor stimulant
Potent inhibitor of neuronal uptake of NA, DA and 5-HT
Effects: euphoria, overconfidence, intensified pleasure, increased motor activity
Withdrawal: depression, dysphoria, craving for more
Can be smoked as free base
Toxicity: nasal septum necrosis, dysrhythmias, coronary/cerebral thrombosis

Front 63

LSD - lysergic acid diethylamide

Back 63

Hallucinogen
5-HT2 agonist: inhibits firing of 5-HT neurons in raphe nuclei (inhibitory 5-HT1A autoreceptors)
Sensory stimulation speeds up firing of locus coeruleus more than usual (via 5-HT2 pathway)

Front 64

Ecstasy
MethyleneDimethoxyMethylAmphetamine
(MDMA)

Back 64

Hallucinogen
Positive effects: changes in feelings and emotions, euphoria
Negative effects: muscle tension/jaw clenching, increased sweating, blurred vision
Residual effects: exhaustion, depression, nausea
Death via: hyperthermia, renal failure, muscle breakdown, overheating

Front 65

Alcohol

Back 65

Social drug: CNS depressant
MOA: enhances GABA-mediated inhibition, inhibits voltage gated Ca2+ channels, glutamate receptors
Effects: slurred speech, motor incoordination, dilates blood vessels, cirrhosis of liver, endocrine effects
Treat tolerance/dependence w/: benzodiazepines, clonidine, propranolol

Front 66

Caffeine (methylxanthines)

Back 66

Social drug: CNS stimulation
MOA: inhibits phosphodiesterase (incr. cAMP levels)
Effects: improved mental performance, diuresis, stimulation of cardiac/skeletal muscle

Front 67

Nicotine

Back 67

Social drug
Central effects: incr. alertness, attention, visual acuity, learning, relaxation
Peripheral effects: incr. pulse, BP, vasoconstriction, nausea/vomiting
Tolerance: rapid to peripheral, little to central
Dependence: Stimulates DA reward centres
Treatment: NRT, mecamylamine (antagonist), clonidine

Front 68

Cannabis

Back 68

Social drug
Activate cannabinoid receptors: hippocampus (impairs memory), substantia nigra (motor disturbances), mesolimbic pathways (reward)
Effects: euphoria, relaxation, incr. appetite, incr. pulse, vasodilation, bronchodilation
Tolerance/dependence: minimal
SEs: relatively safe, may precipitate schizophrenia

Front 69

Amphetamines in weight loss

Back 69

Drug treatment
releases NA, DA and 5-HT
Fenfluramine - preferentially affects 5-HT release
Phentermine
Tolerance develops to appetite suppression in a few weeks

Front 70

Orlistat (Xenical)

Back 70

Weight loss drug
Pancreatic lipase inhibitor
Prevents breakdown of dietary fatty acids (less absorption)
Only small amounts absorbed
SEs: abdominal cramps, flatus, faecal incontinence
Well tolerated, supplement fat soluble vitamins

Front 71

Sibutramine (Reductil)

Back 71

Weight loss drug (intended to be an antidepressant)
Inhibits reuptake of 5-HT and NA at hypothalamic sites involved with food intake
High first pass, active metabolites
SEs: dry mouth, constipation, insomnia
CI: hypertension and heart disease (due to NA increase)
(overweight people have risk factors for these)

Front 72

Rimonabant

Back 72

Weight loss drug
CB1 (cannabinoid) receptor antagonist
Reduce trigger of motivation to eat (cf cannabis increasing appetite)
For treatment of obese (BMI>30) people with associated risk factors (type 2 diabetes/dyslipidaemia)
SEs: suicide, depression, MS (drug has been removed)

Front 73

Potential new targets for action (weight loss drugs)

Back 73

Agents that reduce food intake
- inhibitors of 5-HT and NA reuptake in the hypothalamus
- antagonists for other mediators of hunger
- agonist for leptin, AGRP, cholecystokinin etc.
Agents that increase energy expenditure or enhance lipolysis
- agonists of beta-3 receptors

Front 74

Prohibited methods in sport

Back 74

Enhancement of oxygen transfer (blood doping, products that enhance the uptake, transport or delivery of oxygen)
Gene doping
Pharmacological, chemical, and physical manipulation

Front 75

Nandrolone, stanozolol

Back 75

Drugs in sport
Anabolic androgenic steroids (artificial versions of testosterone)
builds muscle, may assist recovery from training/injury
SEs: acne, liver damage, diabetes, high cholesterol, HIV (needles), mood changes
males: shrinking testicles, breast tissue, infertility, decr. sperm production
females: voice deepens, menstrual cycle changes, incr. body hair

Front 76

Tetrahydrogestrinone (THG), desoxy-methyl-testosterone (DMT)

Back 76

Drugs in sport
THG - related to trenbolone and gestrinone
Designer steroid: water soluble, hard to analyse
DMT - intercepted at Canadian border

Front 77

Blood doping

Back 77

Drugs in sport
Withdraw blood and store it (around 1L)
Return blood before event
Dangers: infection, stroke, CHF, hypertension, blood clots

Front 78

Diuretics in sport

Back 78

Drugs in sport
Helps the body lose water and salt (lose weight)
Can be used to produce weak, dilute urine to mask other drugs
Used in weight regulation sports: wrestling, horse racing
eg. frusemide
SEs: dehydration, fainting, dizziness, nausea, cramps

Front 79

Peptide and Glycoprotein Hormones (in sport)

Back 79

Human chorionic gonadotrophin (hCG): banned in males only
Corticotrophin (ACTH): incr. endogenous corticosteroids, mood elevation
Insulin: incr. protein uptake
Growth hormone (hGH): somatotrophin, incr. growth
Insulin-like growth factor (IGF-1)
Erythropoetin (EPO): incr. RBC production
Pituitary/synthetic gonadotrophins (LH): banned in males only