MCBoM- Pharmacology drugs Flashcards

1
Q

Salbutamol

A

For asthma, partial agonist of B2 receptors in lungs (though some action on B1 in heart
Can delay premature labour

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2
Q

Hemicholinium triethylcholine

A

Competes with choline for uptake into presynaptic varicosity at the cholinergic synapse/NMJ, so less ACh made

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3
Q

Vesamicol

A

Inhibits acetylcholine transport into vesicles at the cholinergic synapse

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4
Q

alpha-latrotoxin

A

Depletes vesicles of acetylcholine at the cholinergic synapse

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5
Q

Botulinum toxin

A

Inhibits exocytosis of ACh vesicles at the cholinergic synapse
Treats:
-blepharospasm (involuntary blinking, difficulty opening eyelids)
-focal spasticity
-spasmodic torticollis (neck move to one side)
-urinary incontinence
-improvement in appearance of wrinkles

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6
Q

Acetylcholine, carbachol, muscarine, bethanechol

A

Parasympathomimetics

Non-selective muscarinic receptor agonists

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7
Q

Cevimeline

A

Selective muscarinic 3 receptor agonist

Increases salivary and lacrimal secretion

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8
Q

Atropine, hyoscine

A

Non-selective muscarinic receptor antagonists

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9
Q

Pirenzepine

A

Selective muscarinic receptor antagonist for M1

Treats peptic ulcers

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10
Q

Atropine

A

NON SELECTIVE MUSCARINIC ANTAGONIST

  • premed for anaesthesia
  • treats bradycardia, inhibits M3
  • antispasmodic for gut (IBS etc), inhibits M3
  • counteracts anticholinesterases (organophosphate/ nerve gas poisoning)
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11
Q

Hyoscine

A

NON SELECTIVE MUSCARINIC ANTAGONIST
as with atropine +
motion sickness

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12
Q

Ipratropium

A

-short term relief from asthma, inhibits M3 in lungs

M3 receptor antagonist

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13
Q

Tropicamide cyclopentolate

A

-inhibit M3 receptors in eye causing mydriasis (dilation) and cycloplegia (no accomodation) for eye exams

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14
Q

Tolterodine Darifenacin

A

-inhibits M3 receptors in detrusor muscle to treat urinary incontinence

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15
Q

Histamine

A

Nicotinic receptor agonist

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16
Q

Hexamethonium

A

Nicotinic receptor antagonist

lowers blood pressure as ganglia block

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17
Q

Tubocurarine (curare)

A
NON DEPOLARISING NMJ BLOCKER
Slow onset (5 mins+)
Long duration (1-2 hours)
Not used clinically- side effects are hypotension, bronchoconstriction, tachycardia, anaphylactic reactions (form histamine release)
18
Q

Pancuronium, Vecuronium, Rocuronium

A

NON DEPOLARISING NMJ BLOCKER
Fast onset (2 mins)
30mins-1 hour duration
Used in intensive care for ventilating

19
Q

Atracurium, Cisatracurium, Mivacurium

A

NON DEPOLARISING NMJ BLOCKER
Fast onset (2 mins)
15-30mins duration
Histamine release

20
Q

Suxamethonium

A

ONLY DEPOLARISING NMJ BLOCKER IN USE
Fast onset (1-2 mins)
2-6 mins duration
Not broken down by acetylcholinesterase, by pseudocholinesterase instead
Muscle relaxant for tracheal intubation
Side effects:
-hyperkalaemia from K+ efflux, so heart disarrythmia and cardiac arrest
-bradycardia
-intraocular pressure rise
-prolonged paralysis with some patients (neonates, liver disease, substrates competing for cholinesterase)
-malignant hyperthermia with rare genetic condition

21
Q

Edrophonium

A

Short acting anticholinesterase
Brief association via weak electrostatic forces
Positively charged, so attracted to negative anionic site of acetylcholinesterase, occupies and blocks from acetylcholine (competes with)
Used to diagnose myasthenia gravis (will see return of muscle strength briefly)

22
Q

Neostigmine

A

Medium acting anticholinesterase
As with slow, but more slowly broken down by acetlycholinesterase
Used to treat myasthenia gravis
Used to reverse neuromuscular block by non-depolarising blockers
Pyridostigmine is the same, but less effect at parasympathetic synapses, so fewer side effects

23
Q

Dyflos

A

Irreversible anticholinesterase

Forms strong covalent bond with esteratic site of acetylcholinesterase leading to depolarising block

24
Q

Malathion, agricultural pesticides, nerve gases

A

Organophosphates.
Malathion- to kill head lice
Agricultural pesticides- to induce depolarising block, suicide
Nerve gases- in chemical warfare, induces depolarising block

25
Q

Ephedrine

A

Displacing agent, affecting noradrenergic transmission at postganglionic sympathetic synapses
Competes with NA for uptake 1, so increased NA in synapse
Used to reverse hypotension after spinal/epidural anaesthesia
In decongestant nasal drops- vasoconstriction of mucosal blood vessels, oedema of nasal mucosa
(can - hypertension, tachycardia, reflex bradycardia)

26
Q

Methyldopa

A

Antihypertensive (when other therapies fail)
Competes with NA for uptake 1
Converted to methylnoradrenaline
Released in exocytosis of vesicles
Activates presynaptic alpha 2 receptors which inhibit NA release, so is a false transmitter
Also activate alpha 2 receptors in CNS, so reduced sympathetic drive to CVS, lower bp

27
Q

Guanethidine

A

Noradrenergic neurone blocker
Only used in UK for rapid control of bp in hypertensive emergencies as severe side effects
Unknown mechanism, but prevents release of NA

28
Q

Adrenaline

A

Uses:

  • resuscitation from cardiac arrest (beta 1)
  • anaphylactic shock (beta)
  • CPR- increases heart rate and force (beta 1)
    - reverses vasodilation (alpha 1)
    - causes bronchodilation (beta 2)
  • with local anaesthetics for local vasoconstriction to prolong drug action (alpha 2)
29
Q

Phenylephrine

A

alpha 1 receptor agonist- to increase bp
-Treats nasal congestion (via local vasoconstriction)
-Causes mydriasis for eye examination
-Can treat acute hypotension in an emergency where other measures fail
Side effects: hypertension, tachycardia/reflex bradycardia, reduced perfusion of vital organs

30
Q

Clonidine

A

alpha 2 receptor agonist- to decrease bp
-Treats hypertension
-Used to prevent migraine
Side effects: dry mouth, depression, sedation, bradycardia, sexual dysfunction

31
Q

Isoprenaline

A

Mixed beta receptor agonist
To treat bradycardia or heart block (beta 1) from overdose of beta blocker
Adverse: tachycardia

32
Q

Dobutamine

A

Mixed beta receptor agonist
For support in MI, cardiac surgery or to treat cardiogenic shock (beta 1)
Adverse: tachycardia, increase in systolic bp (alpha 1)

33
Q

Dopamine

A

Mixed beta receptor agonist
For cardiogenic shock (beta 1)
Adverse: vasoconstriction (alpha 1), tachycardia (beta 1)

34
Q

Levadopa

A

To treat Parkinson’s disease
Can cross blood-brain barrier where dopamine can’t
Is converted to dopamine in the CNS
Need to inhibit dopamine production peripherally also with Carbidopa or Benserazide, which cannot cross bbb

35
Q

Phenoxybenzamine, phentolamine

A

Mixed alpha adrenoreceptor antagonists

-For short term management of hypertensive episodes in Phaeochromocytoma

36
Q

Propanolol

A
Beta blocker (mixed beta adrenoreceptor antagonist)
-For angina, arrythmias, MIs, congestive heart failure, hypertension, glaucoma, acute panic attacks
37
Q

KD

A

Dissociation constant

Concentration of drug at which 50% of receptors are occupied

38
Q

Parasymphatholytics

Parasympathomimetics

A

Parasymphatholytics- antagonise psns, so give SNS effects

Parasympathomimetics- mimic effects of psns

39
Q

Pharmacokinetics

A

The way the body deals with drugs

40
Q

Pharmacodynamics

A

The effects of the drug on the body