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PHARMACOLOGY FRCA > CNS drugs > Flashcards

CNS drugs Flashcards

1
Q

what is the difference between MAO enzymes A and B?

A

A found in brain, liver, placenta, GIT and pulmonary endothelium. breaks down 5HT3, NA and dopamine and melatonin

B - found in brain, NOT found in infants. breaks down tyramine, phenylethylramine and dopamine.

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2
Q

give example of MAOI selective for MAO-A?

A

moclobemide
pirlindole

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3
Q

what are the effects of benzos?

A

CNS:
- sedation, reduced REM sleep
- anxiolysis
- hypnosis
- anti epileptic
- anterograde amnesia

muscle relaxation through affects in dorsal horn

CVS and resp
reduced SVR
reduced TV (slight increase in RR)

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4
Q

how do benzos work?

A

bind BDZ1 and BDZ2 receptors which then associate and modulate GABA A to increase opening and conductance of ion channel - increase chloride and hyperpolarisation

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5
Q

does midazolam have any active metabolites?

A

yes - oxazepam

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6
Q

what are the metabolites of diazepam?

A

nordiazepam, temazepam , oxazepam

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7
Q

which of the benzos has the longest eliimination half life?

A

diazepam - 36 hours

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8
Q

what type of molecule is flumazenil?

A

imadazobenzodiazepine

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9
Q

what is the elimination half life of flumazenil?

A

50 mins
significance of this is that may need to repeat dose or give as IV infusion

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10
Q

when is flumazenil contraindicated?

A

long QTc/ QRS prolongation
dont give in mixed overdose e.g. TCA - may precipitate seizures

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11
Q

which sympathetic ganglia are not adjacent to spinal cord (exceptions)?

A

coeliac and hypogastric

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12
Q

which sympathetic fibres leave spinal cord?

A

preganglionic - travel in white communicates (myelinated)
then after ganglion = grey communicates

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13
Q

what ANS branch does stellate ganglia contain?

A

sympathetic

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14
Q

what fibres of the sympathetic nervous system does the sphlanchnic nerve contain?

A

preganglionic

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15
Q

how many divisions of ANS?

A

sympathetic
parasympathetic
(enteric NS - thought to be the 3rd branch)

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16
Q

what is the NT carried by each synapse in autonomic NS?

A

between pre and post ganglionic - ACh and nACh - in both symp and parasym

sympathetic post ganglionic - NA and adrenoceptors
parasympathetic post ganglionic -ACH and mACHR

exception - sympathetic sweat glands - ACh

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17
Q

where is the alpha 2 receptor predominantly located?

A

pre-synaptic

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18
Q

what is the main source of a2 receptors?

A

circulating catecholamines

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19
Q

what does NA do to B2 and A1 receptors on smooth muscle?

A

a1 - vasoconstriction to all smooth muscle except that of GIT
B2 - vasodilation of skeletal, bronchial and uterine smooth muscle

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20
Q

what enzyme is deficient in phenylketonuria?

A

Phenylalanine hydroxylase

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21
Q

which receptor are adrenaline and NA mosly different?

A

Adrenaline and noradrenaline differ mainly in their effects at β2 adrenoceptors, to which noradrenaline has a much lower affinity.

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22
Q

what is the half life of adrenaline?

A

1 to 3 mins

23
Q

what is the effect of ANS on the bladder?

A

sympathetic - relaxes
parasympathetic - contracts

24
Q

what is the effect of ANS on the erection and ejaculation?

A

sympathetic - ejaculation
parasymp - erection

point and shoot

25
Q

what receptors are present in ganglion of parasymp fibres?

A

mostly nicotinic
but can also get muscarinic - exicitatory

26
Q

what is a NANC NT?

A

non adrenergic non cholinergic neurotransmitter.

27
Q

what does anti-cholinergics do to eye pressure?

A

dilate pupil, reduce drainage, increase eye pressures.

28
Q

how does ipratropium work?

A

muscarinic antagonist
bronchodilation
Gq

29
Q

what is clonidine?

A

a2 agonist
this reduces NA release - hypotension
also analgesic

30
Q

where does doxazocin act?

A

a1 blocker
reduces SVR

31
Q

what do CaCB do to CVS system?

A

reduce contractility and CO
reduce HR - reduce conduction through AVN
reduce SVR

32
Q

how do phosphodiesterase inhibitors reduce SVR?

A

cAMP –> PKA –> phosphorylates MLCK –> inhibits muscle contraction.

phosphodiesterase breaks down cAMP
hence inhibiton will inhibit muscle relaxation

33
Q

give examples of 2 PDE (phosphodiesterase) inhibitors that act on CVS

A

milrinone
Levosimendan (ca sensitiser too)

34
Q

what is the effect of PGE inhibitors on cardiac function?

A

improved ionotropy but not immediate

they enhance effects of other ionotropes e.g. adrenaline

35
Q

what is ranolazine?

A

inhibitor of late inward Na current
used in angina

36
Q

can spinal be done with anti-platelet therapy?

A

monotherapy with aspirin - yes no contraindication

ticagrelor - stop 5 days before

37
Q

how long is dual anti-platelet therapy after PCI?

A

6 to 12 months
then aspirin alone

38
Q

which angina meds should/ shouldnt be continued during surgery?

A

statins, aspirin , b blockers , anti htn (except ACE) - continue

ramipril - stop
ticagrelor / clop - stop

39
Q

which ion channel do CaCB effect?

A

L type

40
Q

which vessels do nitrates dilate?

A

veins predominately

41
Q

what do CaCB do to neuromuscular block?

A

prolong

42
Q

which commonly used drug can ranolazine interact with ?

A

ondansetron - both cause long QT

43
Q

what is the mechanism of action of phentolamine?

A

alpha antagonist

44
Q

which vessels do CaCB mostly affect?

A

arterial vasodilation

45
Q

what does phenytoin do to cyp450?

A

inducer

decreases levels - carbemazepine, COCP, warfarin, clopidogrel, steroids, PPI

46
Q

which AED is a P-glycoprotein (P-gp) inhibitors? what does this mean?

A

phenytoin
normally this pump eliminates drugs. hence inhibition increases conc of drugs / absorption.
e.g pf dabigatran

47
Q

which anti-epileptics are least likely to be associated with anti-epileptic hypersensitivity syndrome?

A

levetiracetam
gabapentin
pregabalin
valproate / topimarate

48
Q

what is anti-epileptic hypersensitivity syndrome?

A

rare, potentially fatal

This syndrome typically includes symptoms such as fever, rash, and systemic involvement (e.g., hepatitis, nephritis, and hematologic abnormalities). AEDs most commonly associated with AHS include carbamazepine, phenytoin, phenobarbital, and lamotrigine.

49
Q

when is ICP monitoring in epilepsy advised?

A

In the 4th stage (aka Refractory Status, 30-90 mins)

50
Q

what is the mechanism of action of …
topiramate, vigabatrin, phenytoin, tiagabine and pregabalin?

A

topiramate - glutamate blocker
vigabatrin - Gaba transaminase inhibitor
phenytoin - Na channel blocker
tiagabine - GABA reuptake inhibitor
pregabalin - Inhibition of alpha 2-delta (α2–δ) subunit of voltage-gated calcium channels (VGCC)

51
Q

which drugs inhibit MAO A and B?

A

MAO-I A= moclobemide - reversible
MAO-I B = selegeline and rasagiline - irreversible

Isocarboxazid is a non-selective MAOI that binds irreversibly to MOA-A and MOA-B.

52
Q

which antimicrobial agent has MAOI activity?

A

Linezolid inhibits the action of MAO-A and can interact with MAOI to cause serotonin syndrome.

53
Q

which antipsychotic causes agranulocytosis?

A

clozapine

54
Q

what type of anti-psychotics are chlorpromazine and flupentixol?

A

Chlorpromazine is a typical antipsychotic of the phenothiazine class.

Flupentixol is a typical antipsychotic of the thioxanthene class.

PHARMACOLOGY FRCA (13 decks)

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