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301 Cards in this Set

  • Front
  • Back

Pilocarpine

Parasympathomimetic


Glaucoma and dry mouth relief

Bethanechol

Parasympathomimetic


Increased GI motility, make pee post-op

Carbechol

Parasympathomimetic


Glaucoma, pupillary contraction, make pee post-op



Methacholine

Parasympathomimetic


Bronchospasm

Effects of parasympathomimetics?



M3 EG MP AC BB


- Exocrine gland secretion


- Gut motility


- Miosis via Pupillary sphincter


- Accomodation via Ciliary


- Bronchoconstriction


- Bladder secretion




cGMP second messenger

Edrophonium

Anticholinesterase


Myasthenia gravis diagnosis

Neostigmine


Pyridostigmine

Anticholinesterases


Do not cross BBB


Treat MG and NM block

Physostigmine

Anticholinesterase


PHYxes an atropine overdose


Crosses BBB

Ecothiophate/dyflos

Anticholinesterase


'ThI' used in eye for glaucoma

Donepezil

Anticholinesterase


Don't remember - Alzheimer's

Anticholinesterase side effects


(List 5)

Bradycardia


Hypotension


Excessive secretion


Bronchospasm


GI hypermotility


CNS effects

Atropine

Anticholinergic


Causes mydriasis, treat AChE poisoning

Benztropine


Trinexyphenidyl

Anticholinergic


Parkinson's

Ipratropium

Anticholinergic


Mydriasis, safe in asthma and COPD

Glycopryriulate


Oxybutinin

Anticholinergic


Pee less

Hyoscine


Scopolamine

Anticholinergic


Motion sickness


Reduced airway secretions - for anaesthesia

Actions of alpha-1 adrenoreceptors (post-synaptic)

Pupil dilation (radial fibre constrict)


Blood vessel constriction


Sphincter constriction


Uterine contraction


Ejaculation


Hair erection


Bronchoconstriction (minor)




IP3 DAG

Actions of alpha-2 adrenoreceptors (on nerve terminal)

Reduced cAMP


Reduced lipolysis


Reduced insulin release


Reduced norepinephrine secretion - low HR CO


Reduced salivary secretion


Platelet aggregation


Blood vessel constriction


GI tract relaxation


NA suppression


Transient hypertension, sustained hypotension

Actions of beta-1 adrenoreceptors

cAMP


Increase HR


Increase myocardial contractility


Increase renin


Salivary amylase secretion



Actions of beta-2 adrenoreceptors

cAMP


Smooth muscle relaxation


Bronchodilation


Blood vessel dilatation


More glucose: increased insulin, gluconeogenesis, glycogenolysis


Uterine relaxation

Actions of beta-3 adrenoreceptors

Lipolysis


Thermogenesis

Phenylephrine

a1 selective direct sympathomimetic


Mydriasis, nasal decongestant

Oxymetazoline

Non-selective direct alpha sympathomimetic


Mydriasis, nasal decongestant

Epinephrine

Non-selective direct alpha sympathomimetic


Acts on alpha AT HIGH DOSE


Vasoconstriction (lowered cAMP)


Smooth muscle contraction


Resuscitation





Dipivephrine


Brimonidine

Non-selective direct alpha sympathomimetic


Epinephrine for open angle glaucoma

Clonidine

Alpha-2 selective direct sympathomimetic


Binds in brainstem to reduce NA release


Treats hypertension

Alpha-methyl Dopa

Alpha-2 selective direct sympathomimetic


Stops dopamine formation (NA precursor)


Hypertension

Side effects of direct alpha sympathomimetics?

Hypotension (especially postural)


Tachycardia (B effects)


Dysrhythmia


Reflex bradycardia


Sedation

Isoprenaline

Direct non-selective beta sympathomimetic


Inotropic and chronotropic


Decreases MAP


Treat bradycardia and heart block

Dobutamine

Beta-1 selective direct sympathomimetic


Increased cAMP and cardiac contractility


Treat cardiogenic shock, severe congestive heart failure

Salbutamol

Beta-2 selective direct sympathomimetic


Bronchodilation


Uterine relaxation


Treat asthma

Direct beta sympathomimetic side effects?

Hypokalaemia


Dysrhythmia (B1)


Tremor


Peripheral vasodilation


Reflex tachycardia

Ephedrine


Tyramine


Amphetamine (MDMA)


Cocaine

Indirect sympathomimetics


Cause NA release by displacing it


Nasal decongestion, appetite suppression, CNS stimulation in narcolepsy




NB CHEESE REACTION!

Indirect sympathomimetics side effects?

Hypertension


Tachycardia


Dependence

Phenoxybenzamine

Non-selective alpha adrenergic antagonist


Irreversible and non-competitive


Treat hypertension from phaeochromocytoma and benign prostatic hyperplasia

Phentolamine

Non-selective alpha adrenergic antagonist


Reversible and short-acting


Hypertensive emergencies e.g. phaeochromocytoma

Doxazosin



Alpha-1 selective antagonist


Vasodilation


Treats hypertension

Prazosin

Alpha-1 selective antagonist


Vasodilation


Treat hypertension

Ergot alkaloids


(Ergotamine, ergometrine)

Alpha antagonists


Ergotamine for migraine


Ergometrine for postpartum haemorrhage

Side effects of alpha adrenergic antagonists?

Hypotension


Nasal congestion


Failure of ejaculation


Miosis


Reflex tachycardia


Sodium and water retention (increased renin)

Atenolol

Beta-1 selective antagonist


Cardioselective


Treats hypertension, angina, acute MI, arrhythmia, congestive heart failure

Propanolol

Non-selective beta adrenergic antagonist


Treats glaucoma, thyrotoxicosis, anxiety, hypertension, angina, acute MI, arrhythmia, congestive heart failure

Pindolol

Non-selective beta adrenergic partial agonist


Treats angina and hypertension

Sotalol

Non-selective beta adrenergic antagonist


Treats dysrhythmia, local anaesthetic effect

Carvedilol



Non-selective beta and alpha-1 blocker


Treat congestive heart failure

Labetalol

Non-selective alpha/beta adrenergic antagonist


Treats gestational hypertension and hypertensive crises

Alprenolol


Oxprenolol

Non-selective beta adrenergic partial agonists


Beta blocker action

Timolol

Non-selective beta adrenergic antagonist


Treats glaucoma

Contraindications for beta blockers?

Asthma


Peripheral vascular disease


Diabetes

Side effects of beta adrenergic antagonists?

Fatigue


Bradycardia


Cold extremities


Breathlessness


Exercise-induced hypoglycaemia (diabetics)


Male sexual dysfunction


Lack of cardioselectivity at higher doses

Suxamethonium (succinylcholine)

Depolarising NMJ blocker


ACh receptor agonist


Causes sustained depolarisation


Muscle relaxant in surgery

Depolarising NMJ block side effects?

Bradycardia


Hyperkalaemia


Increased IOP


Malignant hyperthermia

Pancuronium


Atacurium

Non-depolarising NMJ block

ACh receptor antagonist


Muscle relaxant in surgery


Reversed with neostigmine

Tubocurarine

Non-depolarising NMJ block


ACh receptor antagonist


Muscle relaxant in surgery


Reversed with neostigmine

Hexamethonium

Channel blocker of nicotinic receptor


Ganglion blocker


Effect of having no ANS

Trimetaphan

Nicotinic receptor antagonist


Ganglion blocker


Effect of having no ANS

Captopril

ACE Inhibitor


Lower angiotensin II and aldosterone


Increased sodium and water excretion


Treat hypertension, heart failure


Reduce pre- and after-load

Ramipril


Enalapril

ACE Inhibitor


Lower angiotensin II and aldosterone


Increased sodium and water excretion


Treat hypertension, heart failure


Reduce pre- and after-load

ACE Inhibitor side effects?

Dry cough (increased bradykinin)


Hypotension at first


Proteinuria


Angioedema


Taste disturbance


Renal impairment (if renal artery stenosis)


Don't use with potassium-sparing diuretics

Aliskiren

Renin inhibitor


Stops angiotensinogen conversion to angiotensin I


Treats hypertension


Not routinely used

Losartan


Valsartan


Telmisartan


Irbesartan


Candesartan

Angiotensin II receptor antagonists


Similar to ACE inhibs, no cough


Treat hypertension, heart failure, diabetic nephropathy

What are -sartans? What are their side effects?

Angiotensin II receptor antagonists


Hypotension


Renal impairment if renal artery stenosis

Nifedipine

Dihydropyridine L-type calcium channel blocker


Acts systemically


Treats hypertension, angina



Amlodipine



Dyhydropyridine L-type calcium channel blocker


Acts systemically


Treats hypertension, angina



Verapamil

Phenylakylamine L-type calcium channel blocker


Mainly cardioselective


Slows HR, negative inotropy, antidysrhythmic, treats hypertension, reduces myocardial oxygen demand


Don't use with B-blockers

Diltiazem

Benzothiazepine L-type calcium channel blocker


Some systemic and some cardiac effects


Anti-dysrhythmic, angina, hypertension

Types of calcium channel blockers?


(3 classes)

Dihydropyridine - nifedipine/amlodipine


Phenylakylamine - verapamil


Benzothiazepines - diltiazem

Dihydropyridine calcium channel blocker side effects?

NB Nifedipine and amlodipine


Reflex tachycardia, headache, flushing, swollen ankles

Phenylakylamine calcium channel blocker side effects?

NB Verapamil


Constipation, worsen heart failure, heart block, headache

Benzothiazepine calcium channel blocker side effects?

NB Diltiazem


Bradycardia, headache, flushing, AV block, ankle swelling

Minoxidil

Potassium channel opener


Causes hyperpolarisation


Vasodilation - treats hypertension and hair loss


Usually prescribed with B1 blocker (atenolol) and loop diuretic

Diazoxide

Potassium channel opener


Causes hyperpolarisation and vasodilation


Treats hypertension and hair loss


Usually prescribed with B1 blocker (atenolol) and loop diuretic

Nicorandil

Potassium channel opener


Also has nitrate component


Treats hypertension and angina

Potassium channel opener side effects?

Hypertrichosis (also treat hair loss!)


Hyperglycaemia - lower insulin secretion


Sodium and water retention (action on RAAS)


Reflex tachycardia

GTN


Isosorbide mononitrate



Nitrates


Vasodilation and smooth muscle relaxation


Venodilation


Reduced CO


Treat angina

Nitrates side effects?

Headache, fainting, tolerance, reflex tachycardia (so give B-blockers)

Drugs used in angina treatment?



Nitrates


Calcium channel blockers


Potassium channel openers


Statins


Aspirin


Heparin


Glycoprotein receptor antagonists

Dipyridamole

Thrombus prevention


Increases cAMP


Stops platelet aggregation


Used in those at risk

Ivabradine

Funny channel blocker


Stops Na+/K+ inward current


Reduces heart rate


Treats stable angina, chronic heart failure

Aspirin

Cyclo-oxygenase inhibitor (COX-1 and COX-2)


Lowers platelet aggregation


Anti-inflammatory


Treats pain, those at risk of stroke/MI, angina patients, rheumatoid arthritis

Simvastatin

HMG-CoA Reductase inhibitor


Lowers cholesterol

Heparin

Activates antithrombin III


Inactivates Xa, IXa, XIIa, and thrombin


Anti-clotting


Dose controlled by APTT

Abciximab

Glycoprotein receptor antagonist


Stops clotting


Used in coronary intervention, angina



Tirofiban

Glycoprotein receptor antagonist


Stops clotting


Used in coronary intervention, angina



Acetazolamide (plus side effects!)

Diuretic - carbonic anhydrase (CA) inhibitor


Proximal convoluted tubule


Increased NaHCO3 excretion


Treats glaucoma, heart failure oedema, increased ICP




Metabolic acidosis (less bicarb!)


Renal stones


Alkaline urine


Hypokalaemia

Spironolactone (plus side effects!)



Diuretic - potassium-sparing


Aldosterone antagonist


Acts in late DCT and collecting duct


Inhibits sodium absorption and potassium excretion


Antihypertensive, antialdosterone, antiandrogen




Hyperkalaemia

Amiloride (plus side effects!)

Diuretic - potassium-sparing


Sodium channel blocker


In late DCT and collecting duct


Blocks sodium reuptake


Antihypertensive




Hyperkalaemia

Mannitol


Urea


Glycerine


Isosorbide (plus side effects!)

Osmotic diuretics


Act in PCT


Filtered but not reabsorbed, increase ion and water excretion


Treat raised ICP and acute glaucoma





Furosemide (plus side effects!)

Diuretic - Loop Diuretic


Acts in Loop of Henle


Inhibits NKCC2


Increased Mg/Ca/water excretion


Treat pulmonary oedema in LHF




Hypokalaemia, metabolic acidosis, ototoxicity (reversible), hypomagnesia, hypovolaemia, gout

Bendroflumethiazide (plus side effects!)

Diuretic - Thiazide


Acts in DCT


Inhibits NaCl transport


Increased Na and water excretion


Treat hypertension, oedema, hypocalcaemia, diabetes insipidus




Hypokalaemia, metabolic alkalosis, gout, hyperglycaemia hyperlipidaemia

Levodopa (plus side effects!)

Dopamine precursor


Converted to dopamine by dopa decarboxylase


Treats Parkinson's




CENTRAL - dyskinesia, schizo-style


PERIPHERAL - nausea, vomiting, hypotension

Carbidopa

L-amino acid decarboxylase inhibitor


Levodopa adjunct


Stops peripheral levodopa breakdown


Does not cross BBB


Treats Parkinson's

Benserazide

L-amino acid decarboxylase inhibitor


Levodopa adjunct


Stops peripheral levodopa breakdown


Does not cross BBB


Treats Parkinson's

Entacapone



Peripheral COMT inhibitor


Levodopa adjunct


Stops levodopa breakdown


Does not cross BBB


Treats Parkinson's

Tolcapone

Central COMT inhibitor


Levodopa adjunct


Stops central levodopa breakdown


Treats Parkinson's

Selegiline

MAO-B inhibitor


Reduces dopamine conversion to DOPAC in brain


Treats Parkinson's and depression

Domperidone

Dopamine (D2) receptor agonist


Acts peripherally on CTZ


Anti-emetic

Bromocriptine

Dopamine (D2) receptor agonist


Used to treat early onset Parkinson's to avoid on-off levodopa effects

Pergolide

Dopamine (D2) receptor agonist


Used to treat early onset Parkinson's to avoid on-off levodopa effetcs

Ropinirole

Dopamine (D2) receptor agonist


Used to treat early onset Parkinson's to avoid on-off levodopa effects

Apomorphine

Dopamine (D1/D2) receptor agonist


Used to treat Parkinson's (with domperidone anti-emetic)

Benzhexol

Anti-muscarinic


Corrects excess cholinergic activity in striatum in early Parkinson's treatment

Benztropine

Anti-muscarinic


Corrects excess cholinergic activity in striatum in early Parkinson's treatment

Amantidine

Antiviral and antiparkinsonian


Blocks viral M2 protein ion channels stopping attachment and penetration


Treats influenza A and Parkinson's



Procaine


Tetracaine


Benzocaine

Amino ester local anaesthetics


Block intracellular sodium channels


Reduce/stop action potentials


Treat local pain

Lidocaine (two clinical uses!)


Bupivacaine


Prilocaine

Amino amide local anaesthetics


Block intracellular sodium channels


Reduce/stop action potentials


Treat local pain


Lidocaine: class 1b antidysrhythmic

Local anasthetics side effects?

Local tissue injury


CNS effects: sedation, light-headedness, anxiety, restlessness, convulsions, visual disturbances, coma, resp. depression, hypotension, hypersensitivity, myocardial depression

Carbemazepine

Sodium channel inhibitor


Antiepileptic and neuropathic pain treatment


Old epileptic drug


First choice for partial seizures also used in tonic-clonic seizures

Phenytoin

Sodium channel inhibitor


Antiepileptic and used in neuralgia


For partial and tonic-clonic seizures


Class 1b dysrhythmic

Sodium valproate

Sodium channel inhibitor and GABA enhancer


Antiepileptic drug


Drug of choice for tonic-clonic seizures, also used in partial

Gabapentin

Calcium channel blocker and GABA enhancer


Antiepileptic and neuralgia drug


Used in partial seizures

Ketamine

NMDA receptor antagonist


Dissociative anaesthesia


Treats neuralgia and anasthetises - common use for children

Morphine

u opiate receptor agonist


In substantia gelatinosa and raphé nuclei


Inhibition of N-type calcium channels


Opening of potassium channels


Pain relief



Codeine

Weak morphine pro-drug


Antitussive, antidiarrhoeal, analgaesic

Pethidine

Opiod agonist


Used during childbirth


Analgaesic

Diamorphine

u opiod receptor agonist


Heroin


Used in severe pain

Central opiate side effects?

Nausea


Vomiting


Cough suppression


Sedation


Respiratory depression

Peripheral opiate side effects?

Miosis (CNIII)


Constipation


Reduced secretion


Histamine release


Bronchospasm

Lamotrigine

Sodium channel inhibitor and glutamate release inhibitor


Newer antiepileptic drug


Used in partial, tonic-clonic and absence seizures

Topiramate

Sodium channel inhibitor and NDMA receptor antagonist


Acts at NMDA glutamate site


Antiepileptic and migraine treatment


Used in partial and tonic-clonic

Ethosuximide

Calcium channel inhibitor


Antiepileptic


Blocks T-type calcium channels


Drug of choice for absence seizures

Vigabatrin

GABA enhancer


Inhibits GABA breakdown


Visual field defects may arise!


Used in partial and tonic-clonic seizures

Actions of benzodiazepines and barbituates in epilepsy?

Modify GABA-A chloride channel


Treat tonic-clonic, absence, status epilepticus (clonazepam)

Clonazepam

Benzodiazepine


Modifies GABA-A calcium channel to enhance GABA


Antiepileptic


Drug of choice in status epilepticus, also used in absence

Tiagabine

Inhibits GABA reuptake


Antiepileptic


Used in partial seizures

Felbamate

NMDA receptor antagonist


Acts at glycine site


Used to treat partial seizures

Drug of choice (plus alternatives) in partial seizures?

Main: Carbemazepine, valproate, phenytoin (Na+ inhib)




Lesser:


Lamotrigine, gabapentin, topiramate (Na+ inhib)


Tiagabine (GABA enhancer)



Drug of choice (plus alternatives) in general, tonic-clonic seizures?

Main: Valproate, carbemazepine




Lesser: phenytoin, lamotrigine, topiramate




(Na+ inhibs)

Drug of choice (plus alternatives) in general absence seizures?

Main: Ethosuximide (Ca+ inhib), carbemazepine




Lesser: valproate, lamotrigine, clonazepam

Drug of choice in status epilepticus?

Clonazepam

Sodium channel blocking antiepileptics?


(3 new and 3 old)

Old:


Carbemazepine


Phenytoin


Valproate




New:


Lamotrigine


Gabapentin


Topiramate

Calcium channel blocking antiepileptics?


(2)

Ethosuximide


Gabapentin

GABA enhancing antiepileptics?


(3 inhibit breakdown, 2 modify GABA-A, 1 inhibits GABA reuptake = 6)

Breakdown inhib.:


Valproate


Vigabatrin


Gabapentin




GABA-A modification:


Benzodiazepines (-pam)


Barbituates (-one)




Reuptake inhib:


Tiagabine

NMDAR antagonising antiepileptics?

Felbamate at glycine site


Topiramate at glutamine site

Chlorpromazine

Phenothiazine


Typical antipsychotic


Antagonises D2, H1, muscarinic ACh and a1 adrenoreceptor


Used in psychosis

Thioridazine

Phenothiazine


Typical antipsychotic


Antagonists D2, H1, mAcH and a1 receptors


Used in psychosis

Flupenthixol

Thioxanthine


Typical antipsychotic


Antagonises D2, H1, mACh and a1 receptors


Used in psychosis

Haloperidol

Butyrophenone


Typical antipsychotic


Antagonises D2, H1, mACh and a1 receptors


Esp in mesocortical and mesolimbic


Used in psychosis

Clozapine

Atypical antipsychotic


5HT2 receptor antagonist, 5HT1A partial agonist


Also antagonise mACh and a1

Olanzapine

Atypical antipsychotic


5HT2 receptor antagonist, 5HT1A partial agonist


Also antagonise mACh and a1

Quietapine

Atypical antipsychotic


5HT2 receptor antagonist, 5HT1A partial agonist


Also antagonise mACh and a1

Risperidone

Atypical antipsychotic


5HT2 receptor antagonist, 5HT1A partial agonist as well as D2 antagonist

Side effects of typical antipsychotics?

Sedation


Dystonia, dyskinesia - basal ganglia dopamine blockade


Hyperprolactinaemia


Dribbling


NB they are also ineffective against negative symptoms

Side effects of atypical antipsychotics?

Dribbling


Visceral weight gain - therefore CVD, DM risk


Neutropaenia


Agranulocytosis (clozapine)


Long QT

Benefits of atypical over typical antipsychotics?


(2)

Treat positive and negative symptoms


Fewer extra-pyramidal side-effects

Aripiprazole (plus side effects!)

Third generation antipsychotic


D2 and 5-HT2A antagonist


5-HT1A partial agonist




Hyperprolactinaemia


Hypercholesterolaemia

Mild forms of mood disorder/mania/bipolar treated with...?

Antiepileptics (valproate, carbimazepine)



Severe forms of mood disorder/mania/bipolar treated with...?

Neuroleptics (antipsychotics)


Lithium



Lithium (plus side effects!)

Severe mania and bipolar disorder


Stops neurotransmitter release




Nephrotoxicity, hypothyroidism, CNS effects

Name the four dopaminergic pathways and their main effect.

Mesolimbic - positive symptoms of psychosis


Mesocortical - negative symptoms of psychosis


Nigrostriatal - extrapyramidal (motor)


Tuberoinfundibular - inhibits prolactin

Chloral hydrate

Hypnotic anxiolytic


Rarely used, sometimes given to help kids sleep

Midazolam

Benzodiazepine


Allosteric modification of GABA-A


Short acting


Hypnotic anxiolytic

Lortemazepam

Benzodiazepine


Allosteric modification of GABA-A


Medium acting


Hypnotic anxiolytic



Diazepam

Benzodiazepine


Allosteric modification of GABA-A


Long acting


Hypnotic anxiolytic

Zopiclone

Hypnotic anxiolytic


Enhances GABA at GABA-A a1 subunit


NOT BENZODIAZEPINE

Zolpiden

Hypnotic anxiolytic


Enhances GABA at GABA-A a1 subunit


NOT BENZODIAZEPINE

Zaleplon

Hypnotic anxiolytic


Enhances GABA at GABA-A a1 subunit


NOT BENZODIAZEPINE

Buspirone

Presynaptic 5-HT receptor agonist


Monoamine modulator


Anxiolytic


Works best on pts never given benzodiazepine

Imipramine

Tricyclic antidepressant


Prevents reuptake of 5-HT and NA


Antagonise a1, mACh, H1

Amytriptylline

TCA


PRevents reuptake of 5-HT and NA


Antagonises a1, mACh, H1


Depression and neuralgia

Clomipramine

TCA


Prevents 5-HT and NA reuptake


Also some effect on dopamine


Antagonises a1, mACh, H1

Doxepin

TCA


Prevents 5-HT, NA reuptake


Antagonises H1, mACh, a1

Side effects of TCAs?

Antimuscarinic - dried mouth, blurred vision, constipation, postural hypotension, urinary retention


Cardiac dysrhythmias

Fluoxetine

SSRI


Blocks 5-HT uptake


Depression

Citalopram

SSRI


Blocks 5-HT uptake


Depression

Sertraline

SSRI


Blocks 5-HT uptake


First line in depression post-MI

SSRI side effects?

Can't eat, can't sleep, can't have sex:


Anorexia


Insomnia


Nausea


Loss of libido


Failure of orgasm

Phenelzine

MAO A/B irreversible inhibitor


Stops 5-HT, NA and dopamine breakdown


Depression

Tranylcypromine

MAO A/B irreversible inhibitor


Stops 5-HT, NA and dopamine breakdown


Depression

Iproniazid

MAO A/B irreversible inhibitor


Stops 5-HT, NA and dopamine breakdown


Depression

Maclobemide

MAO-A selective reversible inhibitor


Stops 5-HT, NA and dopamine breakdown


Depression

Side effects of MAO inhibitors?

Insomnia


Convulsions


Agitation


Postural hypotension


Dizziness


Rare hepatotoxicity

Maprotiline

Selective NA uptake blocker


Depression

Venlafaxine

SNRI


Blocks serotonin and NA uptake


Depression


No antimuscarinic effects!

Mianserin

Atypical antidepressant


a2 antagonist, feedback NA inhibition


Also binds to serotonin receptor


Depression

Mirtazapine

Atypical antidepressant


a2 antagonist, feedback NA inhibition


Also bind to serotonin receptor


Depression

Trazodone

Atypical antidepressant


5-HT reuptake inhibitor and 5-HT2 receptor antagonist (increases 5-HT release)


Depression

Thiopental

Barbituate general anaesthetic (IV)


Potentiates GABA at GABA-A


Fast acting


Induces anaesthesia before reaching equilibrium


Rapid recovery


No nausea or analgaesia

Propofol

General anaesthetic (IV)


Potentiates GABA at GABA-A


Rapid action and recovery, no nausea

Etomidate

General anaesthetic (IV)


For emergency use

Nitrous oxide

Inhaled anaesthetic


Rapid onset, carrier gas for another anaesthetic


Antagonises NMDA at glutamate site

Halothane

Inhaled general anaesthetic


Volatile, slower onset, slow recovery


Potentiates GABA at GABA-A


High blood-air partition co-efficient


Maintains anaesthesia

Enflurane

Inhaled general anaesthetic


Volatile, slower onset, slow recovery


Potentiates GABA at GABA-A


High blood-air partition co-efficient


Maintains anaesthesia

Isoflurane

Inhaled general anaesthetic


Volatile, slower onset, slow recovery


Potentiates GABA at GABA-A


High blood-air partition coefficient


Maintains anaesthesia

Desflurane

Inhaled general anaesthetic


Volatile, slower onset, fast recovery


Low blood-air partition coefficient


Maintain anaesthesia

Sevoflurane

Inhaled general anaesthetic


Volatile, slower onset, fast recovery


Low blood-air partition coefficent


Maintains anaesthesia

General anaesthetic which causes respiratory irritation?

Desflurane

Inhaled anaesthetics which cause respiratory depression? (2)

Enflurane, halothane

Warfarin

Anticoagulant


Interferes with vitamin K reduction


Interactions with enzyme inducers/inhibitors!

Streptokinase

Thrombolytic/fibrinolytic


Danger of allergy

Urokinase

Thrombolytic

Tissue Plasminogen Activator (TPA)

Thrombolytic

APSAC

Thrombolytic

Aminocaproic acid


Tranexamic acid


Aprotonin

Anti-fibrinolytics (stop thrombolytic drugs)

Hydrocortisone

Glucocorticoid


To replace cortisol in deficiency


Anti-inflammatory:


Repress NFkB which produces inflam cytokines


Suppress COX products: PGs, LTs, TXs, PAF, histamine

Prednisolone

Glucocorticoid steroid


Anti-inflammatory:


Repress NFkB which produces inflam. cytokines


Suppress PGs, LTs, TXs, PAF, histamine

Betmethasone

Glucocorticoid sterois


Anti-inflammatory:


Repress NFkB which produces inflam, cytokines


Suppress PGs, LTs, TXs, PAF, histamine

Side effects of hydrocortisone and other steroid anti-inflammatory drugs?

Iatrogenic Cushing's


Immunosuppression


Osteoporosis


Suppression of hypothalamic/pituitary/adrenal function


Hyperglycaemia


Lipolysis

Ibuprofen


Fenbufen

Non-selective COX1/2 inhibitors


NSAID

Naproxen

Non-selective COX1/2 inhibitor

Which COX is the main target and is expressed at inflammatory sites? Which COX is in many locations and causes side effects?

a) COX-2


b) COX-1



Paracetamol

COX-2 selective inhibitor


Pain relief


Not very anti-inflammatory

Infliximab

Anti-TNF antibody

Anti-inflammatory


Used in rheumatoid arthritis


Adalimumab

Anti-TNF antibody


Anti-inflammatory


Used in rheumatoid arthritis

Etanercept

Soluble TNFa receptor


Anti-inflammatory


Used in rheumatoid arthritis

Auranofin

DMARD


Anti-inflammatory

Penicillanine

DMARD


Anti-inflammatory

Chloroquinine

DMARD


Anti-inflammatory


Also antimalarial

Azathioprine



Immunosuppressant

Leflunomide

Immunosuppressant

Ciclosporin

Immunosuppressant

Gold standard treatment for congestive heart failure?


(3)

Carvedilol - B blocker


Spironolactone


ACE-I

Hydralazine

Potassium channel opener


Vasodilator in congestive heart failure, used with isosorbide mononitrate

Main B-blockers in heart failure?

Carvedilol - alpha-1 and beta blocker


Bisprolol

Digoxin

Medium-acting inotrope


Blocks Na/K ATPase


Increased Na and Ca in cell


Increased contractility


Heart failure (esp. alongside AF/flutter)

Digitoxin

Long-acting inotope


Inhibits Na/K ATPase, increasing Na and Ca in cell


Increased contractility


Heart failure (esp. alongside AF/flutter)



Ouabain

Short-acting inotrope


Blocks Na/K ATPase


Increased Na and Ca in cell


Increased contractility


Heart failure (esp. alongside AF/flutter)

Milrinone

Phosphodiesterase III inhibitor


Reduced cAMP breakdown


Positive inotropy, lowered pre- and after-load, vasodilation


Treats unresponsive heart failure or after cardiac surgery

Class IA antidysrhythmics:


- Action


- Drugs (3)


- Dysrhythmias treated

a) Block open sodium channels


b) Quinidine, procainamide, disopyramide


c) Supraventricular and ventricular

Class IB antidysrhythmics:


- Action


- Drugs (2)



a) Block inactivated sodium channels


b) Lidocaine, phenytoin

Class IC antidysrhythmics:


- Action


- Drugs (2)


- Dysrhythmias treated

a) Strong sodium channel blockade


b) Flecainide, encainide


c) Tachyarhythmias, ventricular, prophylaxis for AF

Class II antidysrhythmics:


- Action


- Drugs


- Dysrhythmias treated

a) Beta blockers!


b) Propanolol, metaprolol, atenolol


c) SVT, AF

Class III antidysrhythmics:


- Action


- Drugs


- Dysrhythmias treated

a) Prolongation of action potential and refractory period


b) Amiodarone, sotalol


c) SV and ventricular dysrhytmia

Class IV antidysrhythmics:


- Action


- Drugs


- Dysrhythmias treated

a) Calcium channel blockers


b) Verapamil, diltaizem


c) SVT

Adenosine

Anti-dysrhythmic - unclassified


Activates adenosine receptor in cardiac muscle


Inhibits calcium channels and increases potassium permeability


Slows AV node


Treat SVT

Quinidine

Class 1a anti-dysrhythmic


Blocks open sodium channels


Treats SV and V dysrhythmia

Procainamide

Class 1a anti-dysrhythmic


Blocks open sodium channels


SV and V dysrhythmia

Disopyramide

Class 1a anti-dysrhythmic


Blocks open sodium channels


SV and V dysrhythmia

Flecainide

Class 1C antidysrhythmic


Strong sodium channel blockade


Tachys, V, prophylaxis for AF

Encainide

Class 1C antidysrhythmic


Strong sodium channel blockade


Tachys, V, prophylaxis for AF

Amiodarone (plus side effects!)

Class III antidysrhythmic


Prolongs action potential and refractory period


SV and V dysrhythmia


Emergency use




Photosensitivity, thyroid problems, neuropathy, pulmonary alveolitis

Desmopressin

ADH analogue and V2 receptor agonist


Treats neurogenic DI, nocturnal enuresis


Prophylaxis against bleeding in haemophiliacs

Vasopressin

V1/V2 receptor agonist


Vasoconstrictor


Treat bleeding from oesophageal varices, prophylaxis in haemophiliacs

Felypressin

V1 receptor agonist


Vasoconstrictor


Potentiates local anaesthetic effects, treats bleeding from oesophageal varices, prophylaxis for haemophiliacs

Probenecid

Prevents uric acid resorption acting on weak acid transporter


Treat gout and hyperuricaemia


Maintains [plasma penicillin] in serious infections

Ascorbic acid


Ammonium chloride

Makes urine acidic

Potassium citrate

Makes urine alkaline


Metabolised to potassium bicarbonate

Chlorambucil

Alkylating agent


Alkylates DNA and forms carbonium ions


Cancer

Cyclophosphamide

Alkylating agent


Alkylates DNA and forms carbonium ions


Cancer

Mechlorethamine

Alkylating agent


Alkylates DNA and forms carbonium ions


Cancer

Busulfan

Alkylating agent


Alkylates DNA and forms carbonium ions


Cancer

Melphalan

Alkylating agent


Alkylates DNA and forms carbonium ions


Cancer



Lomustine

Alkylating agent


Urea active unit - nitrosurea


Cancer

Carmustine

Alkylating agent


Urea active unit - nitrosurea


Cancer

Cisplatin

Alkylating agent


Platinum analogue


Cross-links DNA residues


Cancer

Carboplatin

Alkylating agent


Platinum analogue


Cross-links DNA residues


Cancer

Oxaliplatin

Alkylating agent


Platinum analogue


Cross-links DNA residues


Cancer

Methotrexate

Anti-metabolite


Antifolate


Binds to dihydrofolate reductase


Cancer

Mercaptopurine


Thioguanine

Anti-metabolites


Purine analogues


Cancer

Fluorouracil


Capecitabine


Cytarabine

Anti-metabolites


Pyrimidine analogues


Cancer

Taxanes

Plant alkaloids


Interfere with spindle formation/microtubules


Cancer

Etoposide

Plant alkaloid


Interferes with spindle formation/microtubules


Cancer

Vincristine


Vinblastine


Vindestine

Vinca alkaloids (plant alkaloids)


Bind to tubulin


Cancer

Camptothecins

Plant alkaloids


Topoisomerase inhibitors


Cancer

Anthracyclines


Doxirubicin


Idarubicin

Cytotoxic antibiotics


Cancer

Actinomycin


Mitoxantrone


Bleomycin

Cytotoxic antibiotics


Cancer

Aciclovir

Antiviral


DNA polymerase inhibitor


Converted by virus thymidine kinase into a form which inhibits the polymerase


HSV, VSV, EBV, CMV

Ganciclovir (plus side effects!)

Antiviral


DNA polymerase inhibitor


Nucleoside analogue


CMV




Bone marrow depression


Carcinogenic

Tribavirin

Antiviral


DNA polymerase inhibitor


Nucleoside, interferes with viral mRNA

Foscarnet (plus side effects!)

Antiviral


DNA polymerase inhibitor


Pyrophosphate analogue, binds to DNA polymerase




Nephrotoxicity

Zidovudine (plus side effects!)

Antiviral (NRTI)


Nucleotide reverse transcriptase inhibitor


Thymidine analogue, chain terminator




Anaemia, neutropaenia, GI disturbances, rash, fever, insomnia, myopathy...

Azidothymidine (AZT) (Plus side effects!)

Antiviral (NRTI)


Nucleotide reverse transcriptase inhibitor


Thymidine analogue, chain terminator




Anaemia, neutropaenia, GI disturbances, rash, fever, insomnia, myopathy...

Didanosine

Antiviral (NRTI)


Nucleotide reverse transcriptase inhibitor

Zalcitabine

Antiviral (NRTI)


Nucleotide reverse transcriptase inhibitor

Nevaripine

Antriviral (NNRTI)


Non-nucleoside reverse transcriptase inhibitor

Delavirdine

Antiviral (NNRTI)


Non-nucleoside reverse transcriptase inhibitor

Saquinavir

Antiviral


Protease inhibitor (-vir)



Nitronavir

Antiviral


Protease inhibitor (-vir)

Nelfinavir

Antiviral


Protease inhibitor (-vir)

Indinavir

Antiviiral


Protease inhibitor (-vir)

Zanamir

Antiviral

Sialic acid analogue = neuraminidase inhib stopping release


Influenza A and B



Ribavarin

Antiviral


Interferes with viral mRNA


Lassa fever, hepatitis C

Idoxuridine

Antiviral


Thymidine analogue


HSV, VSV



Interferons

Antiviral, anticancer


Induce cellular enzymes that inhibit viral replication


Stop cancer cell replication


Cancer, hepatitis B/C, papillomavirus

Trastuzumab

Monoclonal antibody


Against HER2 receptor


Cancer

Bevacizumab

Monoclonal antibody


Against VEGF (blood vessels)


Cancer

Rituximab

Monoclonal antibody


Against CD20 on B-cells


Blood cancers

Imatinib

Tyrosine kinase inhibitor


Selective for Bcr-Abl


Cancer

Penicillin

Beta lactam antibiotic


Bacteriocidal


Stops transpeptidation in cell wall synthesis


Mimics D-alanine



Cephalosporins

Beta lactam antibiotics


Bacteriocidal


Stop transpeptidation in cell wall synthesis

Vancomycin

Glycopeptide antibiotic


Stops transglycosylation in cell wall synthesis


B-lactam resistance, MRSA, superinfection

Teicoplanin

Glycopeptide antibiotic


Stops transglycosylation in cell wall synthesis


B-lactam resistance, MRSA, superinfection

Ramoplanin

Glycopeptide antibiotic


Stops transglycosylation in cell wall synthesis


B-lactam resistance, MRSA, superinfection

Polymixin

Acts as soap


Bury self in membrane of Gram negative bacteria


Narrow spectrum

Isoniazid

Anti-mycobacterial


Targets mycolic acid synthesis


Bacteriostatic

Ethambutol

Anti-mycobacterial


Stops mycolic acid incorporation


Can penetrate CNS

Sulphonamides (sulfa-)

Antimetabolite antibacterials


Inhibit folic acid production


No DNA and RNA


Bacteriostatic

Trimethoprim

Antimetabolite antibiotic


Inhibits folic acid production


No DNA and RNA


Bacteriostatic

Ciprofloxacin

Quinolone antibiotic


DNA gyrase inhibitor


No unwinding of DNA


Broad spectrum

Nalidixic acid

Quinolone antibiotic


DNA gyrase inhibitor


No unwinding of DNA


Broad spectrum

Rifampicin

Antibacterial


RNA polymerase inhibitor


Bacterioststic

Tetracycline

Antibiotic


Block 30s ribosomal subunit


Bacteriostatic


Broad spectrum

Aminoglycosides (-micin)

Antibiotics


Cause binding of wrong tRNA at 50s/30s


Broad spectrum


Bactericidal

Chloramphenicol

Antibiotic


Binds to 50s subunit


Prevents transpeptidation


Bacteriostatic


Absorbed into CNS

Macrolides (-mycin)

Antibiotic


Bind to 50s ribosomal subunit


Prevent translocation


Bacteriocidal/static


Gram +ve only

Metformin (plus side effects!)

Biguanide anti-diabetic


Increases uptake of glucose by tissues


Suppress appetite




Lactic acidosis


Reduced vitamin B12 absoprtion

Thiazolidinediones (-zone)

Antidiabetic


Activate PPARy and sensitive peripheral tissue to actions of insulin

Carbutamide


Tolbutamide


Gilbenclamide

Sulphonylurea antidiabetics


Block ATPase potassium channels causing beta Cell depolarisation and insulin release

Methimazole


Propylthiouracil


Carbimazole


(plus side effects!)

Thioureylene antithyroid drugs


Inhibit iodination of tyrosine residues




Inhibit granulocyte formation in marrow

Radio-iodine

Antithyroid drug


Given orally as iodide

Thyroxine

Thyroid hormone replacement


Hypothyroidism