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Part 1 Pharmacology > CNS > Flashcards

CNS Flashcards

1
Q

Choline esters

A

direct cholinomimetics
ACh, methacoline, bethacol, carbachol
Poor PO
Hydrophilic, not to CNS
Hyolised GIT

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2
Q

Alkaloid cholinomimetics

A

direct
pilocarpine, muscarine, nicotine
Good PO, lipophilic, go to CNS
renally excreted

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3
Q

Bethanachol

A

choline ester direct cholinomimetic
for paralytic ileus and urinary retetntion

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4
Q

Edrophonium

A

Alcohol inderict cholinomimetic
tensilon test for MG

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5
Q

Physostigmine

A

carbamate indirect cholinomimetic
short T1/2
Crosses BBB
tx atropine OD / cholinergic agitation

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6
Q

Tx cholinergic poisoning

A

pralidoxime
atropine
supportive

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7
Q

Tertiary antimuscarinics

A

atropine, tropicamide, pirenzipine, scopolamine
lipid soluble, cross BBB

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8
Q

Quaternary antimuscarinics

A

glycopyrolate, ipratropium, benztropine
don’t cross BBB

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9
Q

Benztropine

A

quaternary antimuscarininc
doesn’t cross BBB
use in parkinsons
Used in dystonic reactions

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10
Q

Glycopyrolate

A

quaternary antimuscarininc
doesn’t cross BBB
used for excess secretions
Poorly absorbed - F 0.05

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11
Q

Cycloplegics and duration

A

antimuscarinincs, paralysis ciliary muscle
tropicaimide - 15-60m
cyclopentolate - 3-6h
atropine 5-6d

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12
Q

Tx bladder spasm, incontinence

A

oxybutinin - M3 antagonist
solifenacin - more M3 selective
Trospium - less CN effects

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13
Q

Contra indications to atropine

A

BPH precaution
Glaucoma, MG, GI obstruction, paralytic ileus

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14
Q

Alpha 1 agonist

A

phenylephrine

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15
Q

Alpha 2 agonist

A

Clonidine

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16
Q

Beta 1 agonist

A

isoprenaline (1=2), dobutamine

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17
Q

Beta 2 agonist

A

isoprenaline (1=2), dobutamine

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18
Q

Phentolamine

A

reversible alpha 1+2 antagonist
tx pheochromocytoma, skin ischaemia secondary to adrenaline
given IV
phenoxybenzamine PO longer half life (irreversible)

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19
Q

Alpha 1 selective antagonists

A

Tx BPH and HTN
prazosin (T1/2 3h) doxazosin an terazosin (T1/2 12)
F0,6, VD0.6, 98% PB

Tamsulosin alpha 1a more prostate specific

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20
Q

Beta blocker OD

A

dec BP and HR, dec BSL
propranolol - Seizure, prolonged QRS and PR
sotalol - inc QTc
Tx glucagon, atropine and isoprenaline

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21
Q

Beta 1+2 + alpha 1 blockers

A

labetolol, carvedilol

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22
Q

B1+2 blockers

A

Timolol
Propranolol
Nadolol - long T1/2 15h

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23
Q

Selective B1 blockers

A

Atenolol - less well absorbed, renally excreted)
Metoprolol
Esmolol

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24
Q

Glaucoma inc outflow

A

cholinomimetics - pilocarpine
prostaglandins - latanoprost
non selective alpha agonists - epinephrin

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25
Q

Glaucoma dec aqueous humor

A

alpha 2 agonists - brimonidine
Beta blockers - timolol
Diuretics - acetazolamide

AH is BAD

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26
Q

Mechanism local anaesthetic

A

bind intracellular part voltage gated sodium channel in open and active state, inhibits depolarisation

Uncharged crosses membrane, charged active at receptor
In rested state difficult to activate (harder than in inactive state)
sympathetic affected first, then small myelinated fibres

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27
Q

Factors effecting local anaesthetic response

A

inc by inc K
dec by in Ca
Dec by acid
Inc by inc blood flow

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28
Q

Ester vs amide local anaesthetic

A

esters e.g. tetracaine procaine rapidly eliminated inplasma by pseudocholinesteraases
amides e.g. lignocaine metabolised in liver longer T1/2

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29
Q

Camparison half life lical anaesthetic

A

Prilocaine 1.5 - 50%pb vd261
Lidocaine 1.6
Bupicocaine 3.5 - 95%pb
Ropivocaine 4.2 vd47

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30
Q

SE Locals

A

Prilocaine - methaemoglobinaemia
Lidocaine - seizures
Bupivocaine - arrhythmias

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31
Q

SE suxemethonium

A

increased intra abdo pressure
Increased IO pressure
Increased Icp
excess salvation
muscle pain
bradycardia
Increased K+
Malignant hyperthermia

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32
Q

Atracurium

A

isoqunolone non depolarising muscle relaxant
metabolised spontaneously/ by plasma esterases so good in hepatic and renal failure
metabolites can cause seizures
Causes histamine release
! seizures

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33
Q

Half lives muscle relaxants

A

short - 5m sux and mivacurium
mid - 20-40m vec, roc, atracurium
long - >40m panc, tubacurarine

34
Q

Pancuronium

A

steroid non depolarising muscle relaxant
long half life >40
Highly protein bound
Renally excreted (other steroid hepatically)
Increased CO an HR (sympathomimetic)

35
Q

Emergency drugs given down ETT

A

Naloxone
Atropine
Vasopressin
Epinephrine
Lidocaine

36
Q

Mechanism volatile anaesthetics

A

increase threshold for firing via K+ channels therefore reduce neuronal activity

37
Q

Volatile MAC

A

Most to least
NOS
des
sevo
iso
en
halothane
methoxy

n.b. metabolism other way round i.e. methoxy most metabolised

38
Q

AEs volatiles

A

hepatic - halothane
renal - methoxy + en + sevo
megaloblastic anaemia - NOS
inc ICP
inc HR - des + iso
Des best for heart problems

39
Q

Typical antipsychotics

A

D2 antagonists
Phenothiazines - chlorpromazine, fluphenazine (more potent)
Thioxanthines
AUTONOMIC SEs
Butyrophenones - haloperidol
EPSEs

40
Q

Atypical antipsychotics

A

5HT2 antagonists
greater effect on negative symptoms

41
Q

Thioridazine

A

typical antipscyhotic
most fatal in OD, inc QTc

42
Q

Drug increasing lithium conc

A

Thiazides
AceI + ATII
NSAIDs
Metronidazole
Hyponatraemia
Dehydration

43
Q

Drugs decreasing lithium conc

A

Acetazolamide
Osmotic diuretics
Theophyline
Caffeine

44
Q

Buspirone

A

Non sedating anxiolytic
partial 5HT and A1 agonist
D2 antagonist

45
Q

Mechanism benzos and barbs

A

both bind near GABAa receptor opening chloride channels causing inc GABAnergic inhition
Benzo frequency
Barbiturates length
barbs also inhib glutamate

46
Q

Flumazenil

A

reversal benzos
binds alpha 1 subunit GABAa
reverses except resp
interacts TCAs

47
Q

Benzo with no active metabolites

A

lorazepam

48
Q

Drug increasing level/ duration anaesthetic muscle relaxants

A

gentamicin

49
Q

Metabolism benzos

A

hepatic oxidation via p450 then conjugation to glucoronides

50
Q

Ethanol metabolism

A

via alcohol dehydrogenase and MEOS to acetylaldehyde
via aldehyde dehydrogenase to acetate

51
Q

Fomepezil

A

alcohol dehydrogenase inhibitor

52
Q

Aldehyde dehydrogenase inhibitors

A

Disulfarim
Metronidazol
Trimethoprim

53
Q

Drugs tx ETOH abuse

A

naltrexone - opioid receptor antagonist
acamprosate - NMDA antag, GABA ag
disulfarim - aldehyde dehydrogenase inhibitor

54
Q

Methanol poisoning

A

metabolised by alcohol dehydrogenase to formaldehyde and formic acid
dec VA, seizures, brady
treat with ETOH and fomepezol

55
Q

Ethelyne glycol poisoning

A

via alcohol dehydrogenase to glycoaldehyde -> glycolic acid -. oxalic acid
calcium oxalate in kidneys - renal tubular necrosis, hypocalcaemia
high anion gap acidosis
formic acid - toxic to retina
Tx ETOH, fomepezol, bicarb, dialysis

56
Q

MAOIs in parkinsons

A

Mainly MAOb but some a action a high dose
Rasagaline selegeline
adjuvant to levodopa
CI with SSRIs an TCAs risk seratonin syndrome

57
Q

COMTi

A

Entacapone
decreases levodopa breakdown peripherally
does not enter CNS
prolongs levodopa action
increases tox levodopa
tolcapone - hepatotoxic

58
Q

Benztropine

A

Muscarininc antagonist in basal ganglia
reduces tremor and rigidity in parkinsons

59
Q

Antiemetic in parkinsons

A

domperidone - doesn’t cross BBB

60
Q

Ergot derivatives

A

ergotamine
agonist 5HT3 and A1
causes vaso constriction
!! risk MI, gangrene, ischaemic bowel from prolonged vasopspasm

61
Q

Tryptan mechanism

A

5HT1 agonist
- cranial artery vasoconstriction
- inhibit nerotransmission
- inibitis neuro inflam peptides

62
Q

Thioridazine

A

Typical antipsychotic
Increases QTc
Most potent

63
Q

Na valproate PK

A

A: po/iv
D: small vD 0.15,T1/2 9-18h, 90%PB

64
Q

Examples TCAs

A

imipramine, amitryptaline

65
Q

Example MAOi

A

mocelbamide, phenelzine, selegeline

66
Q

Barbiturate excretion

A

in urine completely metabolised, except phenobarbitone - 30% unchanged

67
Q

Chlorpromazine SE

A

postural hypotension, impotence and failure to ejaculate
Cholestasis

68
Q

Antiepileptic causing hyponatraemia

A

carbemazepine

69
Q

Half life atropine

A

2h
cycloplegic effects 6-7days

70
Q

Beta blocker low vD

A

atenolol - not lipid soluble
otherwise mainly high vD

71
Q

Contraindication phenobarbital

A

porphyria

72
Q

T1/2 midazolam, diazepam

A

M: 2-4h (tmax 15-20m)
D:20-80h
(tmax 1-2h)
Weak bases, absorbed in SI

73
Q

Amantadine

A

increases dopamine synthesis and release
antiviral
Not metabolised

74
Q

Dopamine agonists

A

bromocriptine (ergot), pramiprexole, ropinarole

75
Q

Carbidopa

A

inhibits AAD (peripheral metabolism ldopa)
reduces dose ldopa by up to 75%, increases amount crosses BBB

76
Q

Levodopa interactions and CI

A

MAOi - hypertensive crisis
B6 - inc peripheral decarboxylation
CI - psychosis, angle closure glaucoma, PUD, melanoma

77
Q

Benzos short half life

A

zolpidem and triazolam

78
Q

Local anaesthetic pK

A

8-9
cations when injected
Works on open na channels

79
Q

Treatment absence seizures

A

ethosuximide
sodium valproate
clonazepam

80
Q

Duration withdrawal benzodiazepines

A

2 weeks plus

Part 1 Pharmacology (13 decks)

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