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FRCA Final > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

Sotalol

A

A non-selective beta blocker with additional class I and III antiarrythmic properties. A racemic mixture, with the D-isomer conferring its class III activity, whilst L-isomer has beta blocking and class III activity. Prolongs the AP and refractory period, and is more effective in maintaining sinus rhythm following DC cardioversion than other beta blockers. 2% of those being treated for sustained VF/VT will go into torsades. 90% oral bioavailibility and not metabolised, water soluble so excreted unchanged by the kidney. Dose adjustment is needed in renal impairment

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2
Q

Which antibiotics are bacteriocidal?

A
  • Very - Vancomycin
  • Finely - Fluroquinolones
  • Proficient - Penicillins
  • At - Aminoglycosides
  • Cell - Cefalosporins
  • Murder - Metronidazole
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3
Q

Carbaprost

A

A prostaglandin F2-alpha analogue used to promote uterine contraction. May cause hypotension, tachycardia and bronchospasm. Otherwise known as haemabate. Avoid in asthma.

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4
Q

Piperacillin

A

Anti-pseudomonal penicillin only available IV

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5
Q

Hyoscine

A

A potant anti-sialogue with some anti-emetic properties (hence it crosses the BBB). Additionally used as sedative and amnesic. Presented as racemix, only L-hyoscine is active. Extensively metabolised by liver esterases (only 1% is excreted unchanged), oral bioavailability highly variable but poor (10-50%). Can be used as a patch behind the ear for motion sickness, although takes >12 hours for effect to occur

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6
Q

Hydralazine

A

Acts to promote ARTERIOLAR smooth mucle cGMP and hence decrease Ca causing arteriole vasodilitation. Undergoes acetylation in the liver, which shows significant pharmacogenetic variation. Crosses the placenta and can cause a foetal tachycardia. Can cause lupus like syndrome (blood dyscrasias and peripheral neuropathies)

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7
Q

Allopurinol

A

A xanthine oxidase inhibitor.

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8
Q

Isocarboxazid

A

A hydrazine non-selective irreversible MAO-I (starting with I). Inhibit hepatic enzymes and may cause hepatotoxicity. Interacts with Pethidine to cause cerebral irritability, hyperpyrexia and CVS instability.

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9
Q

Trimetaphan

A

A quaternary ammonium ganglion blocker used to produce hypotensive anaesthesia. It is a competitive antagonist at all nicotinic ganglion receptors, including those of the adrenal cortex. Side effects are myriad and result mainly from blockade of parasympathetic system. Short half life of only 2 minutes. Direct vasodilating effect on peripheral vessels. Histamine release, significant enough to cause bronchospasm, but probably not responsible for its hypotention. CBF is maintained provided pre-load is kept up and MAP maintained >50. DOES NOT cross the BBB. Implicated in meconium ileus of the newborn and therefore DOES cross the placenta. Is inactivated by plasma cholinesterase and therefore inhibits the metabolism of suxamethonium (by acting as a competitive substrate).

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10
Q

Nefopam

A

A Non-opiod, non-NSAID analgesic of the benzoxazocine class. Useful in postoperative shivering and as an opioid sparring agent. Can cause anticholinergic side effects.

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11
Q

Nifedipine

A

A dihydropyridine calcium channal antagonist. Available as oral (60% bioavailability) or sublingual preparation. Used in angina prophylaxis, hypertension and raynaud’s. Does not affect rate of recovery of L-Ca channel in SAN and does not delay conduction through the AVN So OK to use with a beta blocker. 90% protein bound. Half life 5 hours. Inactive metabolites are excreted in the urine

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12
Q

Levosimendan

A

An “inodilator”. Works by increasing sensitivity of troponin C to calcium, causing increased inotropy. Causes peripheral vasodilitation that reduces pre and after load

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13
Q

Reserpine

A

Centrally and peripherally acting by preventing storage vesicles incorporating noradrenaline from cytoplasm. As a result, NA is rapidly broken down by cytoplasmic MAO and hence stores are depleted. This leads to hypotension from reduced SVR and CO. Side effects include sexual dysfunction, hyperprolactinaemia, gynacomastia, galactorrhoea.

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14
Q

Milrinone

A

Bipridine derivative selective phosphodieserase III inhibitor. Used in the treatment of heart failure. Cause peripheral vasodilitation. 70% protein bound and long half life of 2 hours. Excreted up to 80% unchanged in the kidney so dose adjustment is necessary in renal impairment. Incompatible with frusemide when given via the same cannula. Increased mortality when used in patients with severe heart failure.

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15
Q

Esmolol

A

A non-selective beta blocker (although beta-1 predominates, beta-2 is only seen at high dose) used in the treatment of hypertension/tachycardia under anaesthesia. Has an extremely short half life of only 10 minutes due to rapid hydrolysis by red cell esterases to inactive acid metabolite and methyl alcohol. Does NOT potentiate suxamethonium. No intrinsic sympathomimetic activity. Vd 3.5 l/kg. 60% protein bound.

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16
Q

Pindolol

A

A NON-SELECTIVE Beta-blocker with partial beta-agonist activity. It also has partial agonist / antagonist activity at the 5-HT1A receptor.

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17
Q

Summarise the mechanism of action of the main antibiotics:

  • Penicillins
  • Cephalosporins
  • Carbapenems
  • Vancomycin
  • Chloramphenicol
  • Clindamycin
  • Linezolid
  • Macrolides
  • Tetracyclines
  • Aminoglycosides
  • Sulphonamides
  • Trimethoprim
  • Fluroquinolones
  • Daptomycin
  • Metronidazole
A
  • Competative inhibition of transpeptidase
    • Penicillin, Cephalosporins, Carbapenems
  • Binds to D-alanine D-alanine to prevent transpeptidation prior to the action of penicillin
    • Vancomycin
  • Bind 50S Ribosome subunit to prevent translocation
    • Chloramphenicol, Clindamycin, Linezolid, Macrolides
  • Bind 30S ribosome subunit to prevent transfer of tRNA (prevents elongation) causes misreads:
    • Tetracyclines, Aminoglycosides
  • Sulphonamides
  • Trimethoprim
  • Fluroquinolones
  • Daptomycin
  • Metronidazole
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18
Q

Ephedrine

A

Mixed direct/indirect acting alpha/beta sympathomimetic (also found naturally in some plants). Causes some inhibition of MAO, potentiating NA. Causes unacceptably poor cord pH in obstetric population. Can treat hypotension, bronchospasm, nocturnal enuresis and narcolepsy. 4 sterio-isomers, only the L-isomer is active. Often presented as a racemix. Well absorbed orally. T-half 4 hours (as not metabolised by MAO or COMT). 65% excreted unchanged in urine. Subject to tachyphylaxis.

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19
Q

Phenazosin

A

Opiod agonist, with mixed agonist/antagonist properties

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20
Q

Nateglinide

A

Stimulates insulin release

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21
Q

Azapropazone

A

A discontinued NSAID. Has a half-life of approximately 20 hours and is not extensively metabolised

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22
Q

Aminophylline

A

A preparation of theophylline and ethylenediamine.

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23
Q

Ecothiopate

A

An organophosphate used topically for the treatment of glaucoma. Also causes myosis. Unique to the organophosphates in containing a quaternary nitrogen that also binds to the anionic site of acetylcholinesterase.

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24
Q

Dopexamine

A

Synthetic analogue of dopamine. It acts mainly at Beta-2 and D-2 receptors, it has minimal activity at Beta-1 and D-1. It has no alpha activity whatsoever. Inhibits uptake-1, promoting NA. Rapidly cleared with a half life of 7 minutes

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25
Q

Adrenaline

A

An endogenous catecolamine. Beta effects predominate at low doses, Alpha effects occur at high doses. L-isomers are 15x more potent. Diastolic blood pressure can fall secondary to beta-2 associated vasodilatation.

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26
Q

Isoprenaline

A

A POTENT synthetic catecholamine that acts at BETA-1 and BETA-2 receptors. May cause a fall in MAP secondary to its beta-2 effects causing vasodilitation. Despite this, it increases myocardial oxygen requirements owing to its Beta 1 effect.

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27
Q
A
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28
Q

Benorylate

A

An ester of paracetamol and aspirin

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29
Q

Haloperidol

A

A first generation (typical) antipsychotic of the butyrophenone class. Acts as an antagonist at multiple receptors, particularly D2 (in the CTZ to promote anti-emesis), Alpha adrenergic and mAch. Side effects include increased prolactin production, hypothermia, hypotension, anticholinergic side effects (although generally limited) and extra-pyramidal side effects, which includes parkinsonian like syndromes, and the neuroleptic malignant syndrome.

30
Q

Promethazine

A

An antihistamine anti-emetic with significant sedative side effects, so often used as a premedicant. Well absorbed orally, but subject to a high first pass metabolism in the liver, rendering its oral bioavailibility at 25% (similar to morphine). Duration of action is around 3-6 hours, with metabolites entirely eliminated in the urine.

31
Q

Which anaesthetic agents should you avoid in epilepsy?

A
  • Ketamine (contentious)
  • Etomidate
  • Enflurane (produces epileptiform activity)
  • Alfentanyl (enhances EEG activity)
  • Meperidine (metabolites are proconvulsant)
  • Tramadol (lowers seizure threshold)
  • Sux (if peri-seizure as can increase K+)
  • Anti-emetics with extra-pyramidal side effects
32
Q

Sumatriptan

A

5-HT1 AGONIST used in the treatment of acute migrane and cluster headache

33
Q

Phenoxybenzamine

A

A non-selective alpha blocker used in the treatment of phaochromocytoma

34
Q

Carboprost (Haemabate)

A

Prostaglandin F2-alpha used to stimulate uterine contraction, by potentiating the uterotonic effect of oxytocin. Causes bronchoconstriction, hypotension and tachycardia. Used to treat postpartum haemorrhage due to uterine atony in patients unresponsive to ergometrine and oxytocin. Dose: 250mcg by deep i.m. injection. Direct intramyometrial injection of Carboprost has a faster onset of action. This dose may be repeated but after at least 15 minutes in severe cases. The total dose should not exceed 2 mg (8 doses). Cautions: History of glaucoma or raised intra-ocular pressure, uterine scars; excessive dosage may cause uterine rupture

35
Q

What is the common mechanism of action for anti-epileptic drugs (AEDs)?

A
  • Suppress excitatory neurones (Glutamergic or Na)
  • Enhance inhibitory neurones (GABAergic)
36
Q

Ergometrine

A

Agonist at alpha-1 adrenoceptors, 5HT and dopaminergic recptors. Used to aid delivery of the placenta or help gain control of PPH with an atonic uterus. Causes hypertension and vomiting and should not be used in pre-eclampsia.

37
Q

Atenolol

A

Non selective beta blocker with increased water solubility, so metabolised by the kidney.

38
Q

Methyldopa

A

An analogue of L-DOPA acting as a false substrate for dopa-decarboxylase, thus resulting in the formation of a false neurotransmitter.

39
Q

Tiamterine

A

Works in the distal tubule to inhibit sodium resorption in exchange for potassium and hydrogen ions (i.e. a potassium sparring diuretic similar to spironolactone)

40
Q

Digoxin

A

A cardiac glycoside with positive inotropic effects secondary to an increase in intracellular calcium levels. Inhibits Na/K-ATPase. Slows AV nodal conduction resulting in ventricular rate control in AF. Less than 10% undergoes metabolism in the liver. Primarily excreted unchanged via the kidney by glomerular filtration and tubular secretion, hence the necessity for dose adjustment in renal impairment. Has a long elimination half-life of 35 hours, which is increased by renal impairment.

41
Q

Aspirin

A

An irriversible inhibitor of COX-1. Inhibits renal tubular secretion of URATE.

42
Q

Tranexamic Acid

A

An antifibrinolytic drug. A synthetic analogue of the amino acid lysine. It binds to plasminogen on its lysine binding sites, preventing plasmin formation, and also displaces plasminogen from thrombin. Additionally, it may improve platelet function and have anti-inflammatory effects (inhibits complement activation, monocytes, and neutrophils). In the CRASH-2 trial there was a significant reduction in mortality (1.5%) if given within 8 hours. In elective surgery patients at risk of thromboembolism may increase this risk. The evidence for this is patchy and therefore a risk assessment of all patients should be undertaken before administration. The dose is 1-1.5 g given by slow intravenous injection. If injected too quickly, it causes significant hypotension.

43
Q

Clozapine

A

An atypical antipsychotic working as a partial agonist at D2 receptors, amongst myriad other receptors. Known to cause agranulocytosis so regular blood monitoring is mandatory

44
Q

Clonidine

A

A partial agonist at both ALPHA-1 and 2 receptors (200:1 affinity for alpha 2:1). Reduces MAC up to 50%. Inhibits the release of ADH

45
Q

Can atracurium be used in epilepsy?

A

Yes. A metabolite laudanosine is theoretically epileptogenic although this effect has not been observed in humans. It is however considered good practice to use an alternative.

46
Q

Diazoxide

A

A VASODILATOR chemically related to thiazide diuretics. Used in hypertensive emergencies associated with renal disease, intractable hypoglycaemia and malignant islet cell tumours. Hypotension is mediated by reducing cAMP. Increased glucose due to inhibition of insulin secretion. Also increases catecolamine release. Hyperglycaemia lasts longer than the hypotensive effects. Classically causes arteriolar vasodilatation with minimal affect on the capacitance vessels (postural hypotention is NOT a problem). Increases levels of glycose, catecholamines, renin and aldosterone. May cause fluid retention (despite its relation to a thiazide)

47
Q

Imipramine

A

A tricyclic antidepressant causing a greater degree of postural hypotension than other drugs in its class. Metabolised in the liver to form nortriptyline and desipramine. It is contraindicated in glaucoma. TCA note: Main mechanism of action via competitive blockade of uptake 1 for NA and 5HT causes. Blockade of muscarinic, histaminergic and alpha-adrenoreceptors leads to their non-specific and broad side effects. Typically they are well absorbed, highly lipid soluble, highly protein bound. Metabolism is typically hepatic, but shows significant variability between patients.

48
Q

Oxytocin

A

An oligopeptide structurally similar to ADH and possesses ADH-like activity. Used to promote uterine contraction in failure to progress and following delivery at c-section. Water intoxication may occur, especially when administered with large volumes of intravenous 5% glucose. Decrease in blood pressure occurs within 30 seconds of administration, particularly if given rapidly. Arrhythmias may ensue, most commonly sinus tachycardia, sometimes with ST changes on the ECG. Care is required in parturients with heart disease. Should be administered after delivery by slow bolus of 5 units, then by infusion if required.

49
Q

Rosiglitazone

A

A thiazolidinedione; activates peroxisome proliferator-activated receptor gamma (PPAR-gamma) within the cell nucleus to regulate the genes responsible for glucose and lipid metabolism. As a result, increases sensitivity of peripheral tissues to insulin. May cause fluid retention (avoid in heart failure). Extensively metabolised by the CYP450 system in the liver. Produces inactive metabolites, secreted in the urine. Troglitazone was withdrawn due to hepatitis, so patients on this medication must have regular liver function.

50
Q

Enoximone

A

Imidazole derivative; a selective phosphodiesterase III inhibitor. An “inodilator”. Similar effect to milrinone. Stored 5-8 degrees, and presented in a plastic syringe (glass causes crystal formation). Takes 30 minutes for effect to occur. Typically used in CCF/low CO associated with cardiac surgery. CO rises 30%, LVEDP falls 30%. Oxygen extraction unchanged (lower LV wall tension versus improved coronary blood flow). Shortens refractory time. May trigger further ischaemia in IHD. Well absorbed, but extensive 1st pass metabolism. T-half 7.5 hours, 70% protein bound.

51
Q

Ketanserin

A

A 5-HT2 Receptor antagonist, with particularly high affinity for the 5-HT2-alpha subgroup.

52
Q

Naltrexone

A

A Competative opioid receptor antagonist

53
Q

Phenelzine

A

A hydrazine non-selective irreversible MAO-I (starting with P). Inhibit hepatic enzymes and may cause hepatotoxicity. Interacts with Pethidine to cause cerebral irritability, hyperpyrexia and CVS instability.

54
Q

Metformin

A

An anti diabetic drug of the biguanide class. Works to increase peripheral glucose utilisation. Does not cause hypoglycaemia.

55
Q

Dobutamine

A

A direct acting synthetic catecholamine derivative of isoprenaline. Predominately Beta 1, with some Beta 2 (and Alpha 1 to an even smaller degree). Reduces LVEDP via its action on beta 2 receptors. Used in myocardial stress testing.

56
Q

Droperidol

A

A dopamine antagonist anti-emetic of the butyrophenones class. Avoid in parkinsons disease.

57
Q

Disopyramide

A

A Class 1A anti arrhythmic (Na channel blocker causing PROLONGATION of the AP). Causes a centrally mediated hypotention. No peripheral activity. Suppresses ventricular extrasystoles. CAN cause some ventricular tachycardia, VF or Torsades.

58
Q

Labetalol

A

A mixed alpha/beta blocker with greater affinity for beta receptors (1:3 following oral administration and 1:7 following IV administration!). Has significant sympathomimetic activity. Can cause retrograde ejaculation secondary to its alpha effects

59
Q

Amitriptyline

A

A TCA. Inhibits catecholeamine re-uptake.

60
Q

Which antibiotics are bacteriostatic?

A

We’re ECSTaTiC to be bacterioSTATIC

  • E - Erythromycin
  • C - Clindamycin
  • S - Sulphonamides
  • T - Tetracycline
  • T - Trimethoprim
  • C - Chloramphenicol
61
Q

Ritodrine

A

A moderately selective beta 2 agonists used to arrest premature labour. Crosses the placenta and can cause foetal tachy. Other associations include: FATAL maternal pulmonary oedema, hypokalaemia, hyperglycaemia, vommitting and seizures.

62
Q

Prilocarpine

A

A non-selective muscarinic receptor agonist (parasympathomimetic alkaloid) used in the treatment of dry mouth and glaucoma.

63
Q

Dopamine

A

An endogenous catecolamine. Acts via D1, D2 and Beta receptors. At low doses beta effects predominate, Alpha effects occur at high doses. Does not cross the BBB, although causes nausea and vomitting via action on D1 receptors in the CTZ. Inhibits prolactin secretion. Causes vasodilitation of the mesenteric and renal vascular beds. Increases AV conduction. It has a short half life of 3 minutes, and is metabolised via MAO and COMT to 3,4-dihydroxyphenylacetic acid and homovanillic acid.

64
Q

Ranitidine

A

H2 receptor antagonist. Reduces gastric secretion of H ions. Has NO effect on gastric motility.

65
Q

Verapamil

A

Phenylalkylamine calcium channel antagonist. A derivative of papaverine. DOES affect rate of recovery of L-ca channel in SAN and delays conduction through AVN (better for treating SVTs than nifedipine). Should NOT use with a beta blocker as greater risk of complete heart block. Although well absorbed, undergoes extensive first pass metabolism to yield an oral bioavailibility of only 10%. 70% protein bound and largely excreted by the kidney.

66
Q

Tranylcypromine

A

A non-hydrazine non-selective irreversible MAO-I, probably the most dangerous as also posses significant stimulant activity. Inhibit hepatic enzymes and may cause hepatotoxicity. Interacts with Pethidine to cause cerebral irritability, hyperpyrexia and CVS instability.

67
Q

Nitric Oxide

A

A potent vasodilator. Synthesised from L-arginine. The haemoglobin molecule has an affinity 1500 times higher to this substance than to carbon monoxide. Nitrosyl haemoglobin is produced, which in the presence of oxygen, is oxidised to methaemoglobin.

68
Q

Pioglitazone

A

A thiazolidinedione; activates peroxisome proliferator-activated receptor gamma (PPAR-gamma) within the cell nucleus to regulate the genes responsible for glucose and lipid metabolism. As a result, increases sensitivity of peripheral tissues to insulin. May cause fluid retention (avoid in heart failure). Extensively metabolised by the CYP450 system in the liver. Produces some active metabolites, secreted in the faeces and urine. Troglitazone was withdrawn due to hepatitis, so patients on this medication must have regular liver function.

69
Q

Phenytoin

A

A class 1b antiarrhythmic drug which enhances AV nodal conduction. Metabolised by hydroxylation in the liver, a pathway that is easily saturable just above therapeutic levels. Even mild increases in dose result in zero order kinetics. Has a narrow therapeutic index and it is important to check plasma levels in order to avoid toxicity. Plasma protein binding is about 90%. Crosses the placenta and causes fetal hydantoin syndrome, with craniofacial abnormalities, growth retardation, cardiac defects and mental retardation. Induces mixed function oxidases and increases metabolism of benzodiazepines and warfarin.

70
Q

Metoclopramide

A

A benzamide anti-emetic active at D2 and 5HT receptors (the latter, particularly in high doses). A pro-kinetic effect is mediated by a cholinergic final pathway, and hence this aspect is antagonised by atropine.

71
Q

Flumazenil

A

A competitive inhibitor of benzodiazepines at the benzodiazepine binding site on the GABAA receptor.

FRCA Final (21 decks)

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