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FRCA Guide Qs 2003 > Pharmacology 2003 > Flashcards

Pharmacology 2003 Flashcards

1
Q

Bioavailability of a drug may be influenced by:

  • hepatic extraction
  • gut wall metabolism
  • apparent volume of distribution
  • systemic clearance
  • gastric acidity
A

TTFFT

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2
Q

Nitric oxide

  • is a gas at normal temperatures and pressures
  • is responsible for the pharmacological effects of sodium nitroprusside
  • is produced from L-arginine by NO synthase
  • is derived from the epithelium of blood vessels
  • has an elimination half life of ten minutes
A

TTTTF

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3
Q

Haloperidol can cause:

  • chest wall rigidity
  • Parkinsonian tremor
  • hyperpyrexia
  • beta receptor blockade
  • stimulation of chemoreceptor trigger zone
A

TTTFF

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4
Q

Fentanyl:

  • is 100x more potent than pethidine
  • is less lipid soluble than morphine
  • is a prodrug
  • can cause skeletal muscle rigidity
  • is readily absorbed from the renal tubules
A

FFFTT

-acts directly at the opioid receptor and is lipid soluble, therefore absorbed from the renal tubule

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5
Q

Amethocaine:

  • is hydrolyzed by plasma cholinesterase
  • blocks calcium channels
  • is metabolised to butylamino-benzoic acid
  • can be administered as a 4% gel
  • should not be combined with adrenaline
A

TFTTF

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6
Q

Lidocaine:

  • prolongs duration of cardiac action potential
  • has a high hepatic extraction ratio
  • has a lower systemic toxicity than the same dose of prilocaine
  • can cause metHb-aemia
  • acts by inhibiting the sodium/potassium pump mechanism
A

FTFFF

  • blocks voltage gated fast sodium channels
  • reduces duration and rate of rise of the cardiac action potential
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7
Q

Metronidazole:

  • is absorbed poorly after oral administration
  • is affective against amoebiasis
  • when taken with alcohol may cause abdo pain and flushing
  • does not penetrate the BBB
  • may cause red-brown urine
A

FTTFT

  • completely absorbed after oral administration
  • dark urine is a possible SE
  • can penetrate BBB/breast milk/saliva
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8
Q

Binding of drugs to plasma proteins:

  • increases their pharmacological activity
  • may depend on pH and temp
  • allows rapid renal elimination of the drug
  • retards penetration of the drug through the BBB
  • is similar in the neonate and the adult
A

FTFTF

  • only free drug is filtered at glomerulus
  • protein bound drugs are not available to diffuse through membranes
  • protein binding is reduced in the neonate
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9
Q

Metoclopramide:

  • is a selective D1 receptor antagonist
  • has an action on gastric motility opposed by atropine
  • increases prolactin release
  • is a phenothiazine derivative
  • lowers blood sugar
A

FTTFF

  • metoclopramide acts at D2 and 5HT receptors
  • it’s prokinetic effect is cholinergically mediated and therefore antagonised by atropine
  • it does increase prolactin release
  • it is a benzamine
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10
Q

Substances in the ganglia of the autonomic NS include:

  • ACh
  • noradrenaline
  • 5-hydroxytyptamine
  • butyrylcholine
  • dopamine
A

TFFFF

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11
Q

Etomidate

  • is an imidazole derivative
  • is prepared in propylene glycol
  • is metabolised by esterases
  • has a positive inotropic effect
  • produces excitatory effects that are diminished by opioid premedication
A

TTTFT

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12
Q

The following drugs cause mydriasis when instilled into the conjunctival sac:

  • cocaine
  • ecothiopate
  • amethocaine
  • pilocarpine
  • homatropine
A

TFFFT

  • cocaine and homatropine cause pupillary dilatation
  • cocaine interferes with adrenergic uptake of noradrenaline whilst homatropine is an antimuscarinic
  • ecothiopate, amethocaine and pilocarpine produce pupil constriction
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13
Q

Urinary pH influences reabsorption of drugs from the renal tubule by altering

  • urine volume
  • form of the phosphate buffer
  • ionisation of weak bases and acids
  • tubule cell metabolism
  • active transport in tubules
A

FFTFF

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14
Q

Drugs with a high hepatic extraction ratio include:

  • morphine
  • buprenorphine
  • lignocaine
  • aspirin
  • warfarin
A

TTTFF

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15
Q

Midazolam:

  • becomes highly lipophilic at physiological pH
  • prepared in solution at pH 3-4
  • is hydroxylated in the liver
  • is mainly excreted unchanged by the kidneys
  • antagonises the CNS effects of gamma amino butyric acid
A

TTTFF

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16
Q

The following penicillin compounds are penicillinase resistant

  • phenethicillin
  • flucloxacillin
  • ampicillin
  • cloxacillin
  • benzyl penicillin
A

FTFTF

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17
Q

When using local anaesthetic drugs the max recommended dose for a 70kg patient is:

  • 3mg/kg bupivacaine
  • 20ml of a 1% lidocaine solution
  • 200mg of lidocaine + 1:200000 adrenaline
  • 4ml of a 5% solution of cocaine
  • 200mg of prilocaine
A

FTFFF

  • prilocaine is 6mg/kg without adrenaline or 9mg/kg with
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18
Q

The minimum alveolar concentration of a volatile agent is altered by:

  • pregnancy
  • duration of anaesthesia
  • hyoscine
  • hypothermia
  • alpha2-adrenoceptor agonists
A

TFTTT

  • mac is reduced by 40% in pregnancy
  • mac is reduced by clonidine (alpha 2 agonist)
  • mac is increased by alpha 1 agonists and being pyrexial
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19
Q

The following enzymes help break down noradrenaline:

  • catechol-O-methyl transferase
  • dopamine a-oxidase
  • MAO
  • creatine phosphokinase
  • aspartate transferase
A

TFTFF

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20
Q

Fentanyl:

  • is 100 times as potent as pethidine
  • is less lipid soluble than morphine
  • produces a biphasic respiratory response
  • causes skeletal muscle rigidity
  • is readily absorbed from renal tubules
A

FFTTT

  • it is 1000 times as potent as pethidine
  • may cause delayed resp depression
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21
Q

Drugs with undergo zero order kinetics in normal conditions:

  • phenytoin
  • propranolol
  • tubocurarine
  • ethyl alcohol
  • morphine
A

TFFTF

22
Q

The structure of the following drugs can be reversibly modified by changes in pH:

  • lignocaine
  • midazolam
  • atracurium
  • vecuronium
  • diazepam
A

TTFTF

  • local anaesthetics are weak bases so structure is pH dependent
  • midazolam exhibits pH dependent water solubility but diazepam does not
  • vecuronium has a monoquaternary structure hence its ionisation is pH dependent
23
Q

The following drugs cause mydriasis:

  • morphine
  • cocaine
  • amitriptyline
  • timolol
  • phenylephrine
A

FTTFT

  • phenylephrine, cocaine and amitriptylline are sympathomimetics
  • timolol is a beta blocker used in glaucoma
24
Q

Aspirin:

  • is broken down by esterases
  • OD can cause metHb
  • induces hepatic microsomal enzymes
  • is preferentially eliminated in alkaline urine
  • is CI in children under 12yrs
A

TFFTT

25
Q

The following inhibit the neuronal reuptake of noradrenaline:

  • ephedrine
  • promethazine
  • imipramine
  • aminophylline
  • cocaine
A

FFTFT

  • imipramine and cocaine inhibit reuptake
  • ephedrine enhances NA release
  • promethazine and aminophylline have no effect
26
Q

The following are true of opioid metabolism:

  • morphine 3 glucuronide is an analgesic
  • morphine 6 glucuronide is a ventilatory depressant
  • alfentanil has pharmacologically active metabolites
  • diamorphine has distribution half life of less than 5 mins
  • norpethidine is excitatory to the CNS
A

FTFTT

27
Q

Imipramine

  • is a benzodiazepine derivative
  • may interact with adrenaline
  • may produce urinary retention
  • is CI in glaucoma
  • inhibits neuronal monoamine uptake
A

FTTTT

  • it is a tricyclic antidepressant inhibiting reuptake of monoamine (mainly NA)
  • it antagonises muscarinic cholinergic receptors and alpha 1 adrenergic receptors
28
Q

Important mechanisms in the termination of action of catecholamines include:

  • oxidative deamination by monoamine oxidase
  • catecholamine uptake by adrenergic nerve endings
  • uptake in smooth muscle
  • metabolism by catechol-o-methyltransferase
  • cleavage by esterases
A

TFFTF

29
Q

Bupivacaine

  • produces depolarization of the nerve membrane
  • has a greater clearance than lidocaine
  • has a higher pK than lidocaine
  • is a racemic mix
  • has a lipid solubility similar to lidocaine
A

FFTTF

30
Q

Haloperidol can cause:

  • chest wall rigidity
  • Parkinsonian termor
  • hyperpyrexia
  • alpha receptor blockade
  • chemoreceptor trigger zone stimulation
A

TTTFF

31
Q

CNS toxicity of amide local anaesthetics

  • is related to site of injection
  • is unaffected by changes in hepatic blood flow
  • correlates poorly with body weight in adults
  • is decreased by premed with diazepam
  • is additive when 2 drugs are used together
A

TFTTT

32
Q

Resistance to non depolarizing muscle relaxants may be produced by:

  • thermal injury
  • phenytoin
  • hypoproteinaemia
  • hypocalcaemia
  • carbamazepine
A

TTFFT

  • hypermetabolic rate of the burn injury can result in an increased renal and hepatic clearance of non depolarising muscle relaxants
  • after a burn there is increased ACh receptor population therefore increasing resistance to NDMR
  • anticonvulsants such as carbamazepine and phenytoin increase resistance to NDMR
  • hypoproteinaemia potentiates the action of NDMRs as does hypocalcaemia
33
Q

Mivacurium

  • blocks autonomic ganglia
  • is antagonised by magnesium
  • is a bisquaternary benzyisoquinolone
  • has active breakdown products
  • penetrates the BBB
A

FFTFF

  • no discernable action on muscarinic receptors
  • magnesium potentiates NDMRs
  • does not cross BBB
34
Q

Dilatation of the pupil:

  • improves drainage of aqueous humour
  • occurs to accommodation to near vision
  • will occur if ACh-erase is inhibited
  • occurs when circulating adrenaline concentrations increase
  • is caused by paralysis of smooth muscle supplied by the sympathetic nerves to the eye
A

FFFTF

  • drainage is improved by constriction of pupil
  • anticholinesterase applied to the eye will cause miosis
  • accommodation results in constriction of the pupil
  • adrenaline causes dilator pupillae to contract resulting in myadriasis
35
Q

The MAC of an inhaled agent:

  • is decreased by clonidine
  • may be expressed as volume %
  • is increased in pyrexia
  • is lower in males than females
  • can be predicted by oil/water solubility
A

TTTFF

  • potency is related to oil/gas partition coefficient
36
Q

Isoflurane:

  • has an oil/gas partition coefficient of around 91 at 37C
  • is partially metabolised to trifluoroacetic acid
  • has a MAC value of 1.15% in oxygen
  • is a racemic mixture
  • has a blood/gas partition coefficient of 2.3
A

TTTTF

37
Q

Bupivacaine:

  • has a chiral centre
  • is less potent than procaine
  • is an enzyme inhibitor
  • is hydrolyzed in the plasma
  • is stable in solution
A

TFTFT

  • potency of a local anaesthetic is directly related to it’s lipid solubility, bupivacaine is more lipid soluble than procaine
  • amides are metabolised in the liver
  • most amides contain a chiral centre
38
Q

Therapy with IV mannitol may cause:

  • hyponatraemia
  • low osmolality of plasma
  • an increased blood volume
  • hyperkalaemia
  • delayed increase in ICP
A

TFTFT

39
Q

Propofol

  • is formulated in propylene glycol
  • is highly protein bound in blood
  • has antiemetic properties
  • is conjugated in the liver to glucuronides and sulphates
  • has a low hepatic clearance
A

FTTTF

  • has a high hepatic clearance
40
Q

The blood/gas partition coefficient of an inhalational agent:

  • correlates with anaesthetic potency
  • increases with decreasing temperature
  • is proportional to SVP
  • indicates rapidity of induction of anaesthesia
  • is altered by changes in FiO2
A

FTFTF

41
Q

Opioid drugs:

  • activate receptors found on ligand-gated ion channels
  • can produce analgesia by a peripheral mechanism
  • produce most of their useful effects by actions at the mu receptors
  • mimic the endogenous peptide substance P
  • are as effective intrathecally as they are systemically
A

FTTFF

  • opioid receptors are G-proteins
  • opioid receptors are manufactured by neurones in the dorsal root ganglion and can be exported peripherally
  • do not mimic substance P but can increase it’s concentration at synapses
  • much more potent intrathecally (10-100 times)
42
Q

Pethidine:

  • has membrane stabilising properties
  • has no active metabolites
  • is a phenylpiperidine
  • has anticholinergic properties
  • is an opiate
A

TFTTF

  • it’s a phenylpiperidine opioid (drug which exerts its effects by combining with opioid receptors)
  • norpethidine is an active metabolite which has convulsant effects
  • pethidine is semisynthetic with structural similarity to atropine and anticholinergic properties
  • it also has a local anaesthetic/membrane stabilising action
43
Q

Methyldopa

  • prevents release of ACh from nerve endings
  • inhibits catechol- O- methyl transferase
  • causes formation of a false transmitter
  • blocks ganglionic transmission
  • causes sleepiness
A

FFTFT

  • methyldopa is an analogue of L-DOPA acting as a false substrate for dopa-decarboxylase, therefore resulting in false transmitter formation
  • it does not affect release of ACh from nerve endings
  • it does not inhibit COMT or block ganglionic transmission
  • does cause sleepiness
44
Q

The following inhibit the neuronal re-uptake of NA:

  • ephedrine
  • promethazine
  • imipramine
  • aminophylline
  • cocaine
A

FFTFT

45
Q

Suxamethonium does not pass significantly across the feto-placental membrane because:

  • of it’s elongated molecular configuration
  • the placenta is rich in cholinesterase
  • it is bound to plasma proteins
  • suxamethonium has a low lipid solubility
  • the blood concentration is never sufficiently high
A

FFFTF

46
Q

Desflurane:

  • has a lower boiling point than enflurane
  • undergoes extensive hepatic metabolism
  • has a similar SVP to halothane
  • has a lower BG partition coefficient than halothane
  • is an isomer of enflurane
A

TFFTF

  • BP of des = 22.8C, BP of halothane = 56.5C
  • BG coefficient is 0.42 compared to 2.4 for halothane
  • desflurane and enflurane are ethers, enflurane has a Cl- atom which desflurane doesn’t have
47
Q

Agents which produce anaesthesia at a partial pressure in the brain of less than 10mmHg (1.3kPa) include:

  • enflurane
  • isoflurane
  • desflurane
  • halothane
  • sevoflurane
A

FTFTF

48
Q

Nitrous oxide:

  • oxidises vit B12
  • maintaines combustion
  • has a critical temp of 32.5C
  • inhibits methionine synthetase activity
  • is less soluble in blood compared to nitrogen
A

TTFTF

  • critical temp is 36.5C
  • 40x more soluble in blood than nitrogen
49
Q

Cocaine:

  • is a vasoconstrictor
  • causes hypothermia in OD
  • is absorbed much more rapidly when mixed with adrenaline
  • is broken down by cholinesterase
  • releases ACh from adrenergic neurones
A

TFFFF

  • blocks neuronal uptake of NA and inhibits MAO
  • adrenergic effects are enhanced and vasoconstriction results
  • body temp may increase owing to increased motor activity coupled with reduced heat loss
  • should not be mixed with adrenaline as it’s a vasoconstrictor, but would slow its absorption
  • cocaine is metabolised by hepatic carboxylesterase
50
Q

Alfentanil:

  • is about 90% unionized at pH 7.4
  • has faster elimination from the body than fentanyl
  • has a smaller Vd than fentanyl
  • is more potent than fentanyl
  • is more protein bound than morphine
A

TTTFT

  • elimination 1/2 life is 1-2h, fentanyl is 2-4hrs
  • volume of distribution at steady state is 0.4-1 L/kg, fentanyl is 3-5 L/kg
  • 92% protein bound, morphine is 20-40%
51
Q

The following drugs are competitive antagonists at 5HT3 receptors:

  • cimetidine
  • metoclopramide
  • omeprazole
  • ketanserin
  • granisetron
A

FTFFT

  • metoclopramide acts mainly at dopamine but does act at 5HT3 at higher doses
52
Q

Captopril

  • enhances hypotensive effects of isoflurane
  • is an angiotensin II receptor blocker
  • causes an increase in plasma renin concentration
  • antagonises chronotropic effects of isoprenaline
  • inhibits breakdown of bradykinin
A

TFTFT

  • increased incidence of hypotension with most agents due to reduced blood volume
  • drugs like losartan act as angiotensin receptor blockers but captopril does not have this effect
  • increased renin due to loss of negative feedback from angiotensin II
  • does not interfere with sympathetic nervous system activity
  • reduced metabolism of bradykinin (may be cause of rare SE of angioedema)

FRCA Guide Qs 2003 (3 decks)

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