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79 Cards in this Set

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Cimetidine (Magicul)
H2 Receptor Antagonist (Peptic Ulcers)
Reduces gastric (acid/pepsin) secretion by blocking H2 receptors.
Crosses BBB - CNS depression/excitation
Inhibits CYP450
Ranitidine (Zantac, Rani 2)
H2 Receptor Antagonist (Peptic Ulcers)
Similar to cimetidine, but more potent and fewer ADR (cannot cross BBB), fewer interactions
Omeprazole (Omepral, Losec, Acimax)
Proton Pump Inhibitor (Peptic Ulcers)
Irreversibly inhibits H+/K+-ATPase (proton pump) in parietal cells
Prodrug, activated by acidity of parietal cells
Misoprostol (Cyotec)
Prostaglandin E1 Analogue (Peptic Ulcers)
Suppresses acid secretion + increases bicarbonate and mucus secretion
ADR: diarrhoea, abdominal pain
Bismuth Chelate
Toxic to H. Pylori (Peptic Ulcers)
Coats Ulcer base, adsorbs pepsin
Enhances PG + bicarbonate secretion
Antacids (Mylanta, Gaviscon)
Neutralise stomach acids
ADRs: acid/base + electrolyte disturbances
Interacts with cimetidine/ranitidine
Metoclopramide (Maxolon) & Domperidone (Motilium)
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)
Types of Laxatives
Osmotic - lactulose
Bulk forming - bran
Lubricant - liquid paraffin
Stimulant Purgatives - bisacodyl, senna
Parasympathomimetics - bethanecol
Antidiarrhoeal drugs
Bulk forming laxatives
Antimotility drugs - opioids, antimuscarinics
Antispasmodics - antimuscarinics (buscopan)
Ulcerative Colitis + Crohn's Disease
Glucocorticoids, sulfsalazine (anti-inflammatories?)
Immunosuppressants (azothioprine, mercaptopurine)
Cholestyramine (Questran) + Colestipol (Colestid)
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
Clofibrate, gemfibrozil (Gemhexal), fenofibrate (Lipidil), ciprofibrate + bezafibrate
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
Fluvastatin (Vastin), Pravastatin (Pravachol, Lipostat), Atorvastatin (Lipitor), Simvastatin (Zocor, Lipex), Lovastatin
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
Nicotinic acid
(Hyperlipidaemia)
Inhibits VLDL production
Activates lipoprotein lipase (break down lipids)
ADRs: flushing, gout, palpitations
Probucol
(Hyperlipidaemia)
Lowers plasma HDL + LDL
Inhibits atherogenesis (antioxidant action reducing LDL oxidation + foam cell formation)
ADRs: GIT effects, ventricular tachycardia
Fluoxetine (Prozac), Buspirone (Buspar), Sumatriptan (Imigran), ergot alkaloids, Tegaserod (Zelmac)
Serotonin Agonists
Fluoxetine (SSRI) - depression + other indications
Buspirone - anxiety
Sumatriptan - migraine
Ergot alkaloids - migraine
Tegaserod - constipation dominant IBS (increase gastric motility)
Methysergide (Deseril), Cyproheptadine (Periactin), Ketanserin, Clozapine (Clopine), Ondansetron (Zofran)
Serotonin Antagonists
Methysergide+Cyproheptadine - carcinoid, migraine
Ketanserin - antihypertensive
Clozapine - schizophrenia
Ondansetron - chemotherapy-induced nausea/vomiting
Sumatriptan (Imigran), Zolmitriptan (Zomig), Naratriptan (Naramig), Eletriptan
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
Ergotamine (Cafergot)
Migraine
5HT1 partial agonist, alpha-1 agonist
Administer prior to attack
SE: potential severe long-lasting vasoconstriction
Methysergide (Deseril)
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
Propranolol (Deralin), Amitriptyline (Endep), Valproic acid (Valpro), NSAIDs
Migraine Prophylaxis
Propanolol - most common for continous prophylaxis
Carbamazepine (Tegretol)
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
Sodium Valproate (Valpro)
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)
Ethosuximide (Zarontin)
Anti epileptic
1st choice against absence seizures
Inihibit T-type Ca2+ channels
May precipitate tonic-clonic
SEs: headache, lethargy, hiccup, euphoria
Phenytoin (Dilantin)
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
Phenobarbitone
Anti-epileptic
Still considered useful for infant seizures
Increases GABA-inhibition, decreases glutamate-excitation
SEs: sedation -> respiratory depression (due to excess GABA)
Benzodiazepines - diazepam (Valium), lorazepam (Ativan)
Anti-epileptic
Given IV for status epilepticus
Enhances GABA transmission
SEs: sedation, tolerance
Vigabatrin (Sabril)
Newer anti-epileptic
For partial seizures
Inhibits GABA transaminase (increasing GABA)
Short half-life, but irreversible inhibition
SEs: visual field defects
Lamotrigine (Lamictal)
Anti-epileptic
For partial + generalised seizures
Blocks Na+ channels
Useful for focal + absence seizures
Quite safe in pregnancy
Topiramate (Topamax)
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)
Gabapentin (Neurontin)
Anti-epileptic
For partial seizures
GABA-analogue, altering its metabolism, non-synaptic release and transport
Relatively safe, few drug interactions
L-dopa + benserazide (Madopar) or carbidopa (Sinemet, Kinson)
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
Cabergoline (Cabaser)
Parkinson's Disease
Ergoline D2 Agonist
Can be first line or partial L-dopa replacement
SEs: nausea, sedation, orthostatic hypotension, heart valve problems
Apomorphine (Apomine)
Parkinson's Disease
Dopamine agonist for when other treatments fail
Start SC dosing in hospital, remove other PD medications
SEs: severe, highly emetogenic
Ropinirole (Repreve)
Parkinson's Disease
Non-ergoline Dopamine-2 agonist
Fewer SEs than other DA agonists
May be neuroprotective
Selegiline (Selgene), Entacapone (Comtan), Amantadine (Symmetrel)
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
Benztropine (Cogentin)
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)
Neuroprotective agents against reactive oxygen species (Alzheimer's disease)
NMDA antagonists - stroke
Riluzole (glutamate modulator) - ALS + HD
Coenzyme Q10 - PD
Donepezil (Aricept)
Alzheimer's disease
Cholinesterase Inhibitor
halflife: 70hrs
Metabolised by 2D6 + 3A4 (interacts w/ ketoconazole)
SEs: nausea, diarrhoea, vomiting, insomnia
CI: peptic ulcer, GI obstruction
Rivastigmine (Exelon)
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)
Galantamine (Reminyl)
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
Possible future targets for Alzheimer's disease?
Statins
NSAIDS
Inhibitors of amyloid beta protein formation and aggregation
- beta/gamma secretase inhibitors
- THC
Riluzole (Rilutek)
Huntington's disease
Inhibits Glu release
NMDA R antagonist
Huntington's disease treatments
Movement disorders
- riluzole + olanzapine
Depression
- SSRIs + mirtazapine
Psychosis and behavioural problems
- atypical antipsychotic drugs
Buspirone (Buspar)
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
Lorazepam (Ativan), temazepam (Temaze), Zolpidem (Stilnox), Diazepam (Valium), Midazolam (Hypnovel), Clonazepam (Paxam)
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)
Zaleplon, zopiclone (Imovane), Zolpidem (Stilnox)
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)
Flumazenil (Anexate)
Benzodiazepine antagonist
Uses: BZ overdose, reverse anaesthesia
Administer IV
SEs: may precipitate anxiety, confusion, nausea
(conformational change in receptor, may act as inverse agonist)
Phenobarbital, Thiopentone (Pentothal)
Barbituates
Non-selective CNS depressants
- sedation -> death
Potent CYP450 inducers
Tolerance/dependence
Phenobarbital: anticonvulsant
Thiopentone: IV anaesthetic
Chlorpromazine (Largactil), thiordazine (Aldazine), fluphenazine (Anatensol)
Phenothiazines (Antipsychotic drugs)
DA-2 Receptor blocker
Low potency
SEs: sedation, neuroendocrine effects, seizures, extrapyramidal symptoms, anticholinergic.
Clozapine (Clopine), olanzapine (Zyprexa)
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
Remoxipride, sulpiride, pimozide, risperidone (Risperdal)
New antipsychotics
Sulpiride: selective D2 block, less extrapyramidal
Pimozide: long acting, 'dirty'
Risperidone: D2 + 5HT2 block, fewer extrapyramidal
Lithium Bicarbonate (Lithicarb)
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
Moclobemide (Arima)
For depression
MAOI (specifically MAO-A)
reversible
less interaction w/food (yeast extract etc.)
Imipramine (Tofranil), Amitryptiline (Endep), Nortryptiline (Allegron)
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)
Fluoxetine (Prozac), Paroxetine (Aropax), Sertraline (Zoloft), Citalopram (Cipramil), Escitalopram (Lexapro), Fluvoxamine (Luvox)
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
Venlafaxine (Efexor), Nefazodone, Reboxetine (Edronax)
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
Bupropion (Zyban)
Dopamine-Noradrenaline Reuptake Inhibitor (DNRI)
Weak antidepressant
Inhibits reuptake of DA + NA
Used as pharmacotherapy for cessation of smoking
St. John's Wort
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
Amphetamine, dexamphetamine, methamphetamine, methylphenidate, fenfluramine
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
Modafinil, atomoxetine
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
Cocaine
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
LSD - lysergic acid diethylamide
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)
Ecstasy
MethyleneDimethoxyMethylAmphetamine
(MDMA)
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
Alcohol
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
Caffeine (methylxanthines)
Social drug: CNS stimulation
MOA: inhibits phosphodiesterase (incr. cAMP levels)
Effects: improved mental performance, diuresis, stimulation of cardiac/skeletal muscle
Nicotine
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
Cannabis
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
Amphetamines in weight loss
Drug treatment
releases NA, DA and 5-HT
Fenfluramine - preferentially affects 5-HT release
Phentermine
Tolerance develops to appetite suppression in a few weeks
Orlistat (Xenical)
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
Sibutramine (Reductil)
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)
Rimonabant
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)
Potential new targets for action (weight loss drugs)
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
Prohibited methods in sport
Enhancement of oxygen transfer (blood doping, products that enhance the uptake, transport or delivery of oxygen)
Gene doping
Pharmacological, chemical, and physical manipulation
Nandrolone, stanozolol
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
Tetrahydrogestrinone (THG), desoxy-methyl-testosterone (DMT)
Drugs in sport
THG - related to trenbolone and gestrinone
Designer steroid: water soluble, hard to analyse
DMT - intercepted at Canadian border
Blood doping
Drugs in sport
Withdraw blood and store it (around 1L)
Return blood before event
Dangers: infection, stroke, CHF, hypertension, blood clots
Diuretics in sport
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
Peptide and Glycoprotein Hormones (in sport)
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