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Part 1 Pharmacology > CNS > Flashcards

CNS Flashcards

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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
Glaucoma dec aqueous humor
alpha 2 agonists - brimonidine Beta blockers - timolol Diuretics - acetazolamide AH is BAD
26
Mechanism local anaesthetic
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
27
Factors effecting local anaesthetic response
inc by inc K dec by in Ca Dec by acid Inc by inc blood flow
28
Ester vs amide local anaesthetic
esters e.g. tetracaine procaine rapidly eliminated inplasma by pseudocholinesteraases amides e.g. lignocaine metabolised in liver longer T1/2
29
Camparison half life lical anaesthetic
Prilocaine 1.5 - 50%pb vd261 Lidocaine 1.6 Bupicocaine 3.5 - 95%pb Ropivocaine 4.2 vd47
30
SE Locals
Prilocaine - methaemoglobinaemia Lidocaine - seizures Bupivocaine - arrhythmias
31
SE suxemethonium
increased intra abdo pressure Increased IO pressure Increased Icp excess salvation muscle pain bradycardia Increased K+ Malignant hyperthermia
32
Atracurium
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
33
Half lives muscle relaxants
short - 5m sux and mivacurium mid - 20-40m vec, roc, atracurium long - >40m panc, tubacurarine
34
Pancuronium
steroid non depolarising muscle relaxant long half life >40 Highly protein bound Renally excreted (other steroid hepatically) Increased CO an HR (sympathomimetic)
35
Emergency drugs given down ETT
Naloxone Atropine Vasopressin Epinephrine Lidocaine
36
Mechanism volatile anaesthetics
increase threshold for firing via K+ channels therefore reduce neuronal activity
37
Volatile MAC
Most to least NOS des sevo iso en halothane methoxy n.b. metabolism other way round i.e. methoxy most metabolised
38
AEs volatiles
hepatic - halothane renal - methoxy + en + sevo megaloblastic anaemia - NOS inc ICP inc HR - des + iso Des best for heart problems
39
Typical antipsychotics
D2 antagonists Phenothiazines - chlorpromazine, fluphenazine (more potent) Thioxanthines AUTONOMIC SEs Butyrophenones - haloperidol EPSEs
40
Atypical antipsychotics
5HT2 antagonists greater effect on negative symptoms
41
Thioridazine
typical antipscyhotic most fatal in OD, inc QTc
42
Drug increasing lithium conc
Thiazides AceI + ATII NSAIDs Metronidazole Hyponatraemia Dehydration
43
Drugs decreasing lithium conc
Acetazolamide Osmotic diuretics Theophyline Caffeine
44
Buspirone
Non sedating anxiolytic partial 5HT and A1 agonist D2 antagonist
45
Mechanism benzos and barbs
both bind near GABAa receptor opening chloride channels causing inc GABAnergic inhition Benzo frequency Barbiturates length barbs also inhib glutamate
46
Flumazenil
reversal benzos binds alpha 1 subunit GABAa reverses except resp interacts TCAs
47
Benzo with no active metabolites
lorazepam
48
Drug increasing level/ duration anaesthetic muscle relaxants
gentamicin
49
Metabolism benzos
hepatic oxidation via p450 then conjugation to glucoronides
50
Ethanol metabolism
via alcohol dehydrogenase and MEOS to acetylaldehyde via aldehyde dehydrogenase to acetate
51
Fomepezil
alcohol dehydrogenase inhibitor
52
Aldehyde dehydrogenase inhibitors
Disulfarim Metronidazol Trimethoprim
53
Drugs tx ETOH abuse
naltrexone - opioid receptor antagonist acamprosate - NMDA antag, GABA ag disulfarim - aldehyde dehydrogenase inhibitor
54
Methanol poisoning
metabolised by alcohol dehydrogenase to formaldehyde and formic acid dec VA, seizures, brady treat with ETOH and fomepezol
55
Ethelyne glycol poisoning
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
MAOIs in parkinsons
Mainly MAOb but some a action a high dose Rasagaline selegeline adjuvant to levodopa CI with SSRIs an TCAs risk seratonin syndrome
57
COMTi
Entacapone decreases levodopa breakdown peripherally does not enter CNS prolongs levodopa action increases tox levodopa tolcapone - hepatotoxic
58
Benztropine
Muscarininc antagonist in basal ganglia reduces tremor and rigidity in parkinsons
59
Antiemetic in parkinsons
domperidone - doesn't cross BBB
60
Ergot derivatives
ergotamine agonist 5HT3 and A1 causes vaso constriction !! risk MI, gangrene, ischaemic bowel from prolonged vasopspasm
61
Tryptan mechanism
5HT1 agonist - cranial artery vasoconstriction - inhibit nerotransmission - inibitis neuro inflam peptides
62
Thioridazine
Typical antipsychotic Increases QTc Most potent
63
Na valproate PK
A: po/iv D: small vD 0.15,T1/2 9-18h, 90%PB
64
Examples TCAs
imipramine, amitryptaline
65
Example MAOi
mocelbamide, phenelzine, selegeline
66
Barbiturate excretion
in urine completely metabolised, except phenobarbitone - 30% unchanged
67
Chlorpromazine SE
postural hypotension, impotence and failure to ejaculate Cholestasis
68
Antiepileptic causing hyponatraemia
carbemazepine
69
Half life atropine
2h cycloplegic effects 6-7days
70
Beta blocker low vD
atenolol - not lipid soluble otherwise mainly high vD
71
Contraindication phenobarbital
porphyria
72
T1/2 midazolam, diazepam
M: 2-4h (tmax 15-20m) D:20-80h (tmax 1-2h) Weak bases, absorbed in SI
73
Amantadine
increases dopamine synthesis and release antiviral Not metabolised
74
Dopamine agonists
bromocriptine (ergot), pramiprexole, ropinarole
75
Carbidopa
inhibits AAD (peripheral metabolism ldopa) reduces dose ldopa by up to 75%, increases amount crosses BBB
76
Levodopa interactions and CI
MAOi - hypertensive crisis B6 - inc peripheral decarboxylation CI - psychosis, angle closure glaucoma, PUD, melanoma
77
Benzos short half life
zolpidem and triazolam
78
Local anaesthetic pK
8-9 cations when injected Works on open na channels
79
Treatment absence seizures
ethosuximide sodium valproate clonazepam
80
Duration withdrawal benzodiazepines
2 weeks plus

Part 1 Pharmacology (13 decks)

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