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Pharm Stuff > Adrenergic pharma > Flashcards

Adrenergic pharma Flashcards

1
Q

Phenylephrine

A
  • alpha-1 agonists
  • vasoconstrictor property
  • nasal decongestant
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2
Q

Clonidine

A
  • alpha-2 agonists

- antihypertensive drug via inhibition of NA release

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3
Q

Dipivefrine

A
  • open-angle “simple” glaucoma treatment
  • acts through alpha-2
  • reduces rate of production of aqueous humour
  • facilitates absorption of aqueous humour through activation of alpha-2 on the veins that drain the canal of Schlemm
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4
Q

Dobutamine

A
  • treatment for congestive heart failure

- beta-1 agonist for cardiogenic shock

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5
Q

Salbutamol

A
  • beta-2 selective agonists
  • asthma treatment
  • > production of bronchodilation
  • premature labour
  • > relaxes uterus and delays premature labour
  • unwanted effects: hypokalaemia, tremor, peripheral vasodilation, reflex tachycardia
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6
Q

INDIRECT ACTING SYMPATHOMIMETICS

A

tyramine, ephedrine and amphetamine

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7
Q

intravenous NA

A

acting mainly via alpha-adrenoceptors -> vasoconstriction -> increased peripheral resistance -> increased BP -> rise in pressure activates baroreceptor reflexes -> reflex bradycardia (reflex vagal stimulation releasing ACh onto muscarinic receptors in the heart) -> slowing of heart rate (despite NA effect at beta-1 receptors)

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8
Q

Isoprenaline

A
  • beta-adrenoceptor selective agonist
  • vasodilation in skeletal muscle and other vascular beds -> fall in BP -> reflex tachycardia
  • direct increase in force and rate of contraction of heart
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9
Q

Ergotamine

A
  • treatment of a migraine in an acute attack

- ergot alkaloids

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10
Q

Ergometrine

A
  • treatment of postpartum haemorrhage

- ergot alkaloids

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11
Q

Hydergine

A
  • cerebral vasodilator
  • treatment of dementia
  • ergot alkaloids
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12
Q

LSD

A
  • lysergic acid diethylamide

- ergot alkaloids

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13
Q

Methysergide

A
  • 5HT receptor antagonist/agonist
    – migraine treatment
  • ergot alkaloids
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14
Q

Bromocriptine

A
  • DA receptor agonist (D2)
    – galactorrhea and parkinsonism treatment
  • ergot alkaloids
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15
Q

Phentolamine

A
  • reversible competitive antagonist at alpha

- short acting

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16
Q

Propanolol

A
  • reversible competitive receptor antagonist at beta
17
Q

Phenoxybenzamine

A
  • irreversible non-competitive antagonist
  • acts by forming covalent with alpha
  • long-acting
  • characterised by reduction in slope of log-dose response curve and decrease in the max response to an agonist
18
Q

Oxprenolol, Pindolol

A
  • partial agonist of beta, but can antagonise effects of full agonist (e.g. NA)
19
Q

Prazosin, Doxazosin

A
  • antagonist selective for alpha-1
20
Q

Propranolol and Atenolol

A
  • beta- adrenoceptor antagonist
  • selective for Beta-1 (cardioselective)
    (atenolol non-selective)
21
Q

Sotalol

A
  • beta- adrenoceptor antagonist

- local anaesthetic action

22
Q

Carvedilol and Labetatol

A
  • beta- adrenoceptor antagonist

- alpha-adrenoceptor antagonist properties

23
Q

Major contraindications of beta- adrenoceptor antagonist

A

ASTHMATICS, in which they cause bronchospasm

Other contraindications:

  • AV block
  • several peripheral vascular disease
  • diabetes
24
Q

Therapeutic uses of beta-adrenoceptor antagonists

A

angina, hypertension, glaucoma, myocardial infarction, arrhythmias, thyrotoxicosis, CHF, anxiety and for prophylaxis (protective treatment) of migraine

25
Q

Unwanted effects of beta- adrenoceptor antagonists

A

fatigue, bradycardia, cold extremities, breathlessness, sleep disturbance, nightmares

26
Q

L-DOPA

A
  • increases rate of synthesis as it by-passes rate-limiting step, which is the conversion of L-tyrosine to L-DOPA by tyrosine hydroxylase
  • used in Parkinsonism
27
Q

Metirosine (alpha-methyltyrosine)

A
  • inhibits enzyme tyrosine hydroxylase and therefore catecholamine synthesis
28
Q

alpha-methyl DOPA

A
  • false transmitter
  • anti-hypertensive agent
  • resistant to degradation by MAO
  • converted by DOPA decarboxylase enzyme (aromatic L-amino acid decarboxylase, enzyme with lack of substrate specificity) to alpha-methyl dopamine, which is subsequently converted by DA-beta-hydroxylase to alpha-methyl-NA (false transmitter, resistant to degradation by MAO because of the alpha-methyl group)
29
Q

Carbidopa

A
  • polar compound
  • a drug that inhibits decarboxylase enzyme (from L-DOPA to DA)
  • used in Parkinsonism
30
Q

Disulfiram

A
  • copper chelating agent

- can inhibit DA-beta-hydroxylase (from DA to NA)

31
Q

Reserpine (and related drugs)

A
  • affect vesicular transporters, leading to depletion of NA by preventing the passage of catecholamines into storage vesicles -> catecholamines escape into cytoplasm of nerve terminal and are inactivated by MAO
32
Q

Tetrabenazine

A
  • short-acting NA and DA depletory (acts on storage)
  • reversible
  • used to treat hyperkinetic movement disorder e.g. Huntington’s disease
33
Q

Guanethidine (and related drugs, anti-hypertensive agents)

A
  • can inhibit NA release mechanism
  • enter via the uptake 1 mechanism and accumulate in sympathetic neurones to block neurotransmission
  • a local anaesthetic blocking Na+ channels
34
Q

Cocaine

A
  • can inhibit uptake 1 mechanism of NA
35
Q

Desmethylimipramine

A
  • tricyclic antidepressant

- can inhibit neuronal uptake 1 mechanism of NA

36
Q

Beta-oestradiol

A
  • can inhibit uptake 2 mechanism of NA
37
Q

Phenelzine

A
  • MAO inhibitors

- non-selective

38
Q

Selegiline

A
  • MAO-B inhibitor

- used in Parkinsonism

39
Q

Entacapone

A
  • COMT (catechol-O-methyl transferase) inhibitor

Pharm Stuff (7 decks)

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