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96 Cards in this Set
- Front
- Back
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Nicardipine |
Dihydropyridine, calcium channel blocker used as antihypertensive treatment, specific to blood vessels' smooth muscle calcium channels. Used for antihypertensive treatment and for angina as well |
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Nimodipine |
Dihydropyridine, calcium channel blocker used as antihypertensive treatment, specific to cerebral blood vessels |
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Verapamil |
Non dihydropyridine, calcium channel blocker specific to myocardial calcium channels, used as antihypertensive treatment. |
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Propranolol |
Non selective beta blocker used as antihypertensive treatment. Also used as an anxiolytic because it reduces tachycardia at the B1 receptor and tremor at the B2 receptor. |
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Pindolol |
Non selective beta blocker with partial agonist activity used as antihypertensive treatment |
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Atenolol |
Beta 1 selective blocker used as antihypertensive treatment, still not safe for asthmatic patients |
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Carvedilol |
Beta blocker with alpha blocker activity, used as antihypertensive treatment |
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Acebutolol |
Beta 1 selective blocker with partial agonist activity, used as antihypertensive treatment |
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Nebivolol |
Beta blocker with extra NO activation because of its nitrogen moiety used as antihypertensive treatment |
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Sotalol |
Beta blocker that also inhibits potassium efflux, allowing the refractory period in myocytes which is helpful for arrhythmia, used as antihypertensive treatment. |
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Phentolamine |
Non selective alpha blocker, also has side effects including diarrhoea and postural hypotension, used as antihypertensive treatment. |
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Prazosin |
Alpha 1 selective blocker used as antihypertensive treatment, also lowers LDL and raises HDL. |
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Methyldopa |
False neurotransmitter, alpha 2 selective agonist used for antihypertensive treatment. Doesn't affect renal or cerebral blood vessels so well tolerated, even in pregnant women. |
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Perindopril, captopril |
ACE inhibitors used as antihypertensive treatment |
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Losartan |
Angiotensin II receptor blocker used as antihypertensive treatment |
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Mannitol |
Osmotic diuretic, increases osmolarity of tubular fluid, reducing water reabsorption in collecting duct |
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Acetazolamide |
Carbonic anhydrase inhibitor, used as a diuretic. Prevents Na+, Cl- and HCO3- uptake into blood vessels in the proximal convoluted tubule, reducing the water that is reabsorbed with it. |
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Furosemide |
Loop diuretic that inhibits the Na+/Cl-/K+ channel in the ascending loop of Henlé, increasing osmolarity of the tubular fluid and reducing water reabsorption in the collecting duct. Used for oedema (general, pulmonary, renal, hepatic or cerebral) or heart failure. |
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Bendroflumethiazide |
Thiazide like diuretic that inhibits the Na+/Cl- channel in the distal convoluted tubule, increasing osmolarity of the tubular fluid and reducing water reabsorption in the distal tubule and collecting duct, used for oedema, cardiac failure or hypertension. Also increases calcium reabsorption in the distal convoluted tubule so used for hypercalcuria and paradoxical nephrogenic diabetes insipidus. |
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Spironolactone |
Potassium sparing diuretic that inhibits aldosterone in the collecting duct, reducing sodium channel reabsorption and potassium excretion. Weakly active on its own and also causes feminisation of the male foetus. Used for oedema or antihypertensive treatment if the hypertension is due to increased aldosterone. |
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Amiloride |
Potassium sparing diuretic that inhibits aldosterone sensitive sodium channels in the collecting duct, reducing sodium reabsorption and potassium excretion. |
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Dabigatran |
Anticoagulant that inhibits factor IIa production. Orally active, used for preventing venous thrombosis. |
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Rivaroxaban |
Anticoagulant that inhibits factor Xa production. Orally active, used for venous thrombosis. |
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Heparin, dalteparin (low MW) |
Anticoagulants that activate antithrombin III, which inhibits factors IIa and Xa. Given IV or subcutaneously in surgical situations to prevent venous thrombosis, otherwise digested in the gastrointestinal tract. |
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Warfarin |
Anticoagulant that inhibits vitamin K in factors IIa, VIIa, IXa and Xa. Used for preventing venous thrombosis but has many side effects. Orally active. |
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Clopidogrel |
Anti-platelet drug that inhibits P2Y12 activation by ADP. Used for arterial thrombosis (preventing stroke or myocardial infarction). |
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Aspirin |
Anti-platelet drug that irreversibly acetylates COX1, reducing thromboxane A2 synthesis and hence GPIIb/IIa expression. Also blocks formation of prostaglandins hence reduces inflammation. Orally active and used for arterial thrombosis or fever/headache. |
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Abciximab |
Anti-platelet drug that antagonises GPIIb/IIIa, used for arterial thrombosis. Given IV or subcutaneously but has many side effects so use is limited and by specialists. |
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Alteplase |
Thrombolytic drug that is a recombinant tissue type plasminogen activator, converting plasminogen into plasmin, and dissolving fibrin clots. Used IV once a clot has already been formed after stroke or myocardial infarction. Very potent and can cause bleeding so only used in emergency situations. |
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Simvastatin |
A statin that has low selectivity to the liver. Inhibits HMG-CoA reductase and reduces cholesterol synthesis. Also reduces macrophage growth and thromboxane A2 and RhoA (increasing NO and increasing endothelial stability). Used for atherosclerosis. |
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Pravastatin |
A statin that has high selectivity to the liver. Also reduces macrophage growth and thromboxane A2 and RhoA (increasing NO and increasing endothelial stability). Used for atherosclerosis. |
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Gemfibrozil |
Fibrate. Used as treatment for atherosclerosis. Activates PPAR alpha and gamma, causing more transcription of LDL, ApoA1&2, and less of ApoC 3. This means more fatty acid oxidation in the liver, and less plasma LDL and triglycerides. In the VA-HIT study it was shown to reduce cardiovascular events but not deaths. |
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Niacin (vitamin B3, nicotinamide) |
Used as treatment for atherosclerosis. Decreases lipase activity in the liver, reducing oxidised LDL and increasing HDL. Increases acute phase proteins, decreasing CRP and fibrinogen. Decreased fibrinogen and oxidised LDL means less macrophage activation and atherosclerotic plaque formation. Doesn't seem to work in the longterm and caused side effects including rashes, pruritus, dry skin and mucous membranes in the HPS2-THRIVE trial. |
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Ezetimibe |
Inhibits cholesterol uptake in the small intestine, probably by inhibiting NPC1L1 after glucuronidation. Used for treating atherosclerosis and hyperlipidemia. In the IMPROVE-IT trial, showed good efficacy with statins in post ACS patients. |
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Torcetrapib |
Cholesterol ester transfer protein inhibitor used for atherosclerosis treatment. Prevents conversion of HDL to LDL, but increased mortality so trial was stopped. |
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Anti PCSK antibodies |
Blocks PCSK from inhibiting LDL receptors and LDL metabolism. Useful in treating atherosclerosis and hypercholesterolemia. |
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Salbutamol |
Short acting beta 2 adrenergic receptor agonist used for treatment of asthma, because it relaxes bronchial smooth muscle and reduces inflammatory mediator production from mast cells. Also used for treatment of uncomplicated premature labour to relax smooth muscle of uterine wall. However can be harmful in diabetic and hyperthyroid patients. |
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Salmeterol |
Long acting beta 2 receptor agonist, that has a long tail chain that can flip in and out of the beta 2 receptor, preventing desensitisation. Also increases the effect of glucocorticosteroids by priming the glucocorticosteroid receptor and cAMP activation of CEBP alpha, which helps glucocorticosteroid binding to its DNA response element. |
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Ipratropium bromide |
Short acting muscarinic receptor antagonist. Has a charged nitrogen moiety that prevents it from diffusing out of the lungs (less systemic side effects). Used for treatment of asthma or obstructive airway disease. Nonselectively blocks M1 (good), 2 (good, bad) and 3 (good) receptors on ganglia and bronchial smooth muscle cells, preventing parasympathetic constriction of airways. |
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Tiotropium bromide |
Long acting muscarinic receptor antagonist. Has a charged nitrogen moiety that prevents it from diffusing out of the lungs (less systemic side effects). Used for treatment of COPD. Selectively blocks M1 (good) and 3 (good) receptors on ganglia and bronchial smooth muscle cells, preventing parasympathetic constriction of airways. |
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Prednisolone, fluticasone |
Glucocorticosteroids used for treatment of inflammation in asthma. Binds to glucocorticosteroid receptor, which becomes active and binds to DNA response elements, causing transactivation (transcription of anti inflammatory mediators but also endocrine side effects) and transrepression (blocking transcription of inflammatory mediators) |
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Theophylline |
PDE and PI3K inhibitor used in treatment for COPD. Reduces histone acetylation and inflammatory gene expression and is used along with glucocorticosteroids. |
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Theobromine |
Cough suppressor derived from cocoa plants, can be used as treatment for COPD. |
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Rimonabant |
Cannabinoid receptor antagonist that can be used for smoking cessation as treatment for COPD. |
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Bupropion |
Non SSRI antidepressant, dopamine and noradrenaline reuptake inhibitor and nicotinic receptor antagonist that can be used for smoking cessation as treatment for COPD. |
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Dopamine |
Could be used as dopamine replacement therapy but causes side effects like nausea, vomiting, impaired renal function, cardiac arrhythmias, so not used for Parkinson's. |
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Metoclopramide |
Can be used in conjunction with dopamine as dopamine replacement therapy for Parkinson's, by preventing nausea side effects of dopamine. But can cross the BBB and worsen extrapyramidal symptoms. |
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L-DOPA |
Dopamine precursor that can be used as dopamine replacement therapy in Parkinson's. But is converted into dopamine in the periphery as well by dopa decarboxylase so causes the same nausea and vomiting side effects as dopamine. |
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Carbidopa |
Can be used in conjunction with L-DOPA for dopamine replacement therapy for Parkinson's, because it inhibits dopa decarboxylase in the periphery so prevents it from being converted into dopamine and having nausea side effects. Effective at first but in the longterm the effect wears off and patients get fluctuations of dyskinesia. |
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Domperidone |
Dopamine D2 & D3 receptor antagonist that prevents dopamine's nausea side effects (in the gastrointestinal tract) for use in Parkinson's but can cause cardiac toxicity. |
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Bromocriptine |
Dopamine receptor agonist, specific to D2 receptors. Has a 5 ergot ring structure but this causes problems with heart valves. Used for treatment of Parkinson's. Longer duration of action that L-DOPA and doesn't require dopaminergic neurons to be present, but because it can affect other dopaminergic pathways, can cause nausea, vomiting, hallucinations. |
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Ropinerol |
Dopamine receptor agonist, specific to D2 receptors. Doesn't have a 5 ergot ring structure but this causes addictive behaviour. Used for treatment of Parkinson's. Longer duration of action that L-DOPA and doesn't require dopaminergic neurons to be present, but because it can affect other dopaminergic pathways, can cause nausea, vomiting, hallucinations. |
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Selegiline |
MAO-B inhibitor used for treatment of Parkinson's. Used early in the disease because it only preserves what dopamine is left. Reduces required dose of L-DOPA. Since it is selective, doesn't cause peripheral side effects. |
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Resagiline |
Non selective MAO inhibitor that is used for treatment of Parkinson's with L-DOPA. Also shown to have anti apoptotic effects (neuroprotective). Early studies showed it might slow disease progression but later studies didn't show this effect. |
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Tolocapone |
COMT inhibitor in CNS and periphery used for treatment of Parkinson's. In the CNS, it stops dopamine metabolism. In the periphery, it stops conversion of L-DOPA into 3-OMD, which usually competes with L-DOPA for transport across the BBB. So more L-DOPA gets into the brain and its required dosage can be reduced. But can have cardiovascular complications. |
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Entacapone |
COMT inhibitor in the periphery used for treatment of Parkinson's. In the periphery, it stops conversion of L-DOPA into 3-OMD, which usually competes with L-DOPA for transport across the BBB. So more L-DOPA gets into the brain and its required dosage can be reduced. But can have cardiovascular complications. |
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Amantadine |
Antiviral that is also used as treatment for Parkinson's. Increases the amount of dopamine released per nerve impulse and reduces its reuptake. Also elevates mood of patient (good for depression), but tolerance develops within 9 months. |
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Deep brain stimulation |
Used as Parkinson's treatment. Electrode is inserted into the brain, and overstimulates the subthalamic nucleus until it shuts down. The subthalamic nucleus usually inhibits dopamine release in the substantia nigra. A pacemaker is attached to the chest and can control the frequency and length of pulses. Very good for treating rest tremor but doesn't work in all patients. |
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Ciclesonide |
Glucocorticosteroid prodrug that is only metabolised into its active form in the lungs so it doesn't have systemic side effects. Used as treatment for asthma. |
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Roflumilast |
PDE4 inhibitor used for treatment of asthma. PDE4 usually catabolizes cAMP (anti inflammatory), so inhibiting it means more cAMP and less inflammation. |
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Thiopentone |
Barbiturate used as an anaesthetic for surgical procedures. Has rapid onset and offset. Acts at the barbiturate receptor protein of the GABA receptor to enhance GABA binding and enhance its opening of the chloride channel by increasing the duration of openings. |
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Amobarbital |
Barbiturate used as a hypnotic for treatment of severe intractable insomnia. Has a half life of 20 hours but has many drug interactions e.g. can potentiate alcohol's inhibitory effect on the brain. Acts at the barbiturate receptor protein of the GABA receptor to enhance GABA binding and enhance its opening of the chloride channel by increasing the duration of openings. |
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Phenobarbital |
Most commonly used barbiturate in developing countries as an anticonvulsant, but not much in developed countries because it can cause death if overdosed. Acts at the barbiturate receptor protein of the GABA receptor to enhance GABA binding and enhance its opening of the chloride channel by increasing the duration of openings. Not used for absence seizures. |
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Diazepam |
Commonly used benzodiazepine as an anticonvulsant, anxiolytic and antispasmodic. Has a half life of 32 hours. Safer than barbiturates. Acts at the benzodiazepine receptor protein of the GABA receptor to enhance GABA binding and enhance its opening of the chloride channel by increasing the frequency of openings. |
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Oxazepam |
Benzodiazepine used as an anxiolytic. Short acting with a half life of 8 hours, and is a metabolite of other benzodiazepines including diazepam and nordiazepam. Safer than other benzodiazepines because it isn't metabolised in the liver so can be used for patients with liver disease. Acts at the benzodiazepine receptor protein of the GABA receptor to enhance GABA binding and enhance its opening of the chloride channel by increasing the frequency of openings. |
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Zopiclone |
Sedative drug of the cyclopyrrolone class. Short acting with a half life of 5 hours. Acts at the benzodiazepine receptor protein to enhance GABA binding. Has similar efficacy as benzodiazepines and less hangover effects, but dependency is still a problem. |
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Buspirone |
Anxiolytic drug that is an agonist of the 5HT1a receptor. Has a slow onset of action (days to weeks) and few side effects. |
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Carbemazepine |
Sodium channel inhibitor to stop glutamate release, for treatment of epilepsy. Locks the sodium channel in an open inactive state and induces hepatic enzymes. Used as frontline treatment for partial seizures. Also used for tonic clinic seizures. |
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Phenytoin |
Sodium channel inhibitor to stop glutamate release, for treatment of epilepsy. Blocks the class 1b sodium channel. Used for most types of epilepsy. |
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Retigabine |
Potassium channel enhancer for treatment of epilepsy. Agonist of the Kv7alpha subunit, which increases potassium influx and hyperpolarisation, preventing the release of glutamate. Only used as adjunctive treatment. |
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Ethosuximide |
T type calcium channel blocker for treatment of epilepsy. Prevents calcium induced glutamate release. Mainly used as frontline treatment for absence seizures. |
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Gabapentin |
Calcium channel blocker for treatment of epilepsy. Thought to inhibit the beta subunit of calcium channels, preventing glutamate release. |
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Levetiracetam |
Inhibitor of the synaptic vesicle associated protein SV2A of glutamate for treatment of epilepsy. Mainly used for partial epilepsy. Safe and effective. |
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Topiramate |
Inhibits the kainate receptor of glutamate for treatment of epilepsy, at the GluK5 subunit. Also affects sodium channels and GABA receptors. Used for most types of epilepsy, and as frontline treatment for myoclonic seizures. |
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Perampanel |
Blocks the AMPA receptor of glutamate for treatment of epilepsy. Used as adjunctive treatment for partial seizures. |
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Felbamate |
Inhibitor of the NMDA receptor of glutamate for treatment of epilepsy. |
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Clonazepam |
Benzodiazepine that is a GABA receptor agonist used for treatment of epilepsy. |
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Tiagabine |
Inhibitor of the GABA transporter protein (GAT1), preventing GABA uptake for treatment of epilepsy. Used as adjunctive treatment for partial seizures. |
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Sodium valproate |
Inhibitor of the GABA transaminase enzyme (GABA-T), preventing GABA metabolism. Used as frontline treatment of all forms of epilepsy. |
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Vigabatrin |
Irreversible inhibitor of the GABA transaminase enzyme (GABA-T), for treatment of epilepsy. Used as monotherapy for infantile spasm or adjunctive for partial seizures. |
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Chlorpromazine
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The initial first-generation antipsychotic, discovered in the 1950s. Antagonist of D2 receptors, so used to treat the positive symptoms of schizophrenia, but has anticholinergic effects e.g. sedation and rarely extrapyramidal side effects (e.g. musculoskeletal due to the nigrostriatal pathway).
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Haloperidol
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First generation antipsychotic used for treatment of schizophrenia. Very potent D2 receptor antagonist (50x more than chlorpromazine). Therapeutic effects develop after 6-8 weeks but it commonly has extrapyramidal side effects due to other dopamine pathways.
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Clozapine
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Second generation antipsychotic that is the most effective drug to treat schizophrenia. Antagonises many receptors: M1, H1, 5HT2a, alpha1. Difficult to understand its mechanism of action because of its many targets. Also useful for treating negative symptoms of schizophrenia, but has many dangerous side effects (fatal neutropenia, agranulocytosis, myocarditis, weight gain) due to its many actions, so only used as a last resort.
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Risperidone
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Second generation antipsychotic used to treat schizophrenia. Very potent antagonist of D2 and 5HT2a receptors, but has many extrapyramidal side effects, including hyperprolactinaemia (possible breast enlargement) due to the tuberoinfundibular dopamine pathway.
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Quetiapine
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Second generation antipsychotic used to treat schizophrenia. Very potent antagonist of H1 receptors. Has less side effects than other antipsychotics.
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Aripriprazole
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Second generation antipsychotic used to treat schizophrenia. Partial agonist of D2 and 5HT1a receptors, which would theoretically be the best treatment option because of differential dopamine levels in the brain (increased in the mesolimbic pathway and decreased in the mesocortical pathway), but actually has the same efficacy as other antipsychotics. Less side effects than other drugs.
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Donepezil
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Reversible acetylcholinesterase (AChE) inhibitor used for treatment of Alzheimer's disease, useful because ACh levels are decreased in Alzheimer's patients, so this prevents its metabolism. Has a long plasma half life so only needs to be taken once a day.
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Rivastigmine
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Pseudoreversible acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitor used for treatment of Alzheimer's disease, useful because ACh levels are decreased in Alzheimer's patients, so this prevents its metabolism. Has a half life of 8h so needs to be taken more than once a day. Has side effects of nausea and vomiting. Also since BChE is important in the liver, could result in liver dysfunction. Has been reformulated as a transdermal patch.
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Galantamine
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Acetylcholinesterase (AChE) inhibitor that also acts as an agonist of nACh receptors, for treatment of Alzheimer's disease. Found and extracted from the flowers in Eastern Europe/Russia. Has a 7hr half life, and is specific to the brain (alpha 7 nAChR) so no musculoskeletal side effects.
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Memantine
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NMDA receptor antagonist used for treatment of Alzheimer's disease, because it's thought that neuroinflammation causes overexcitation using glutamate. Is a use-dependent non-competitive antagonist with low channel affinity for NMDA receptors. Has a long half life, and is used with donepezil. With normal glutamate activity, its slow antagonism (binding and release) doesn't make much difference but with excess glutamate activity, its slow antagonism is very useful at blocking glutamate.
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Tarenflurbil
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(Failed) gamma secretase inhibitor for use in Alzheimer's disease. Binds to the APP molecule and modulates gamma secretase cleavage of it. Also acts as an NSAID, because of its similar structure to ibuprofen. But in clinical trials, had no effect so it was shelved.
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Semagacestat
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(Failed) small molecule inhibitor of gamma secretase for use in Alzheimer's disease. Resulted in many deaths during clinical trials, so discontinued. Possibly due to gamma secretase's role in the Notch pathway in development and tissue homeostasis - many patients in the trial developed skin cancer.
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Beta secretase inhibitors
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Drugs in development for Alzheimer's disease that target the enzyme that cleaves APP in pathology before gamma secretase. However, the enzyme is also important in muscle spindles so it inhibition of it might cause motor side effects.
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Bapineuzumab
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(Failed) humanised monoclonal antibody for against beta amyloid for use in Alzheimer's disease. Didn't work in clinical trials.
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Solanezumab
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(Failed) humanised monoclonal antibody against beta amyloid for Alzheimer's disease, didn't achieve primary outcome but improved a subgroup of patients so further trials are being done.
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Methylene blue
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Tau inhibitor for treatment of Alzheimer's disease. Inhibits tau aggregation. However, is already licensed for treatment of methaemoglobinaemia and pharma companies won't make money out of it so studies keep being delayed.
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