Drugs Acting At The ANS - Adrenergic Receptors. Flashcards

1
Q

What two types of receptors do NA act on?

A

Alpha and Beta. Generally alpha excitation, Beta relaxation of effector cells.

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2
Q

List in order of sensitivity the types of chemicals which react with alpha adrenoreceptors.

A

Noradrenaline>Adrenaline>Isoprenaline.

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3
Q

List in order of sensitivity the types of chemicals which react with beta adrenoreceptors.

A

Isoprenaline>Adrenaline>Noradrenaline.

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4
Q

Effects of Alpha 1 adrenoreceptor stimulation.

A

Vasoconstricion, GI smooth muscle relaxation, Salivary secretion (going to eat) and hepatic glycgenolysis (give energy to eat). NASAL AND OCULAR DECONGESTANTS.

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5
Q

Effects of Alpha 2 adrenoreceptor stimulaiton.

A

Vasoconstriciton (post junctional), Inihibition of transmitter release (pre junctional), inibition of insulin release. Platelet aggregation.

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6
Q

Effects of Beta 1 adrenoreceptor stimulation.

A

Increased cardiac rate and force.

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7
Q

Effects of Beta 2 adrenoreceptor stimulation.

A

Vasodilation in muscle, Brochodilation, Relaxation of visceral smooth muscle, Hepatic glycogenolysis.

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8
Q

Effects of Beta 3 adrenoreceptor stimulation.

A

Lipolysis.

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9
Q

Noradrenaline synthesis.

A

Tyrosine to DOPA, then Dopamine, Noradrenaline and finally Adrenaline.

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10
Q

What drug would you give to increase levels of dopamine in the brain?

A

Levodopa.

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11
Q

How does Levodopa increase levels of Dopamine?

A

Levodopa increase levels of DOPA which is converted by DOPA carboxylase into Dopamine.

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12
Q

What enzymes are involved in the conversion of Tyrosine to adrenaline.

A

Hydroxylase, Decarboxylase, Beta Hydroxylase, Phenylethanoloamine N-methyltransferase.

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13
Q

What should you give along with Levodopa?

A

A peripheral DOPA decarboxylase inhibitor. This should be given to prevent dopamine production in the peripheral nervous system and prevent hyperdopaminergia.

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14
Q

Hyperdopaminergia is associated with what?

A

Schizophrenia.

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15
Q

Reserpine.

A

Blocks vesicle transport of Noradrenaline.

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16
Q

Drugs which affect NA storage.

A

Reserpina, MAO inhibitors.

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17
Q

Drugs blocking the release of NA.

A

Guanethidine, Bretylium, go through uptake 1 and abolish response to nerve stimulation.

18
Q

Drugs which cause NA release even without nerve stimulation.

A

Tyramine, Amphetamines and Ephedrine. Enter via uptake 1, displace NA from vesicles. Cause effects similar to NA in the sympathetic nervous system.

19
Q

Drugs that increase or decrease release of NA?

A

Stuff that affect alpha 2 receptors.

20
Q

Types of MAO inhibitors.

A

Moclobemide - depression, Pargyline, Selegeline - parkinson’s disease.

21
Q

Tyramine cheese reaction.

A

When food containing tyramine is consumed and the patient is taking a MAO inhibitor, there is the chance that the patient may suffer a hypertensive crisis.

22
Q

Problem with MAOI.

A

When ingested orally they affected the digestion of dietary amines.

23
Q

Hypertensive crisis.

A

Malignant hypertension - cause acute impairment of one or more organ systems. The blood pressure should be lowered slowly. SYSTOLIC > 180, DIASTOLIC > 120.

24
Q

Use of pseudoephedrine?

A

Nasal Decongestant.

25
Q

Inhibitors of uptake 1.

A

Tricyclic antidepressants - cocaine, aphetamines and guanethidine.

26
Q

Inhibitors of uptake 2.

A

Some corticosteroids.

27
Q

Effects of uptake inhibitors.

A

Enhance transmission. Creates euphoria.

28
Q

COMT.

A

Catechol-O-methyl transferase. Degrades catecholamines; dopamine, noradrenaline, epinephrine.

29
Q

Alpha 1 antagonist.

A

Zosin, Inhibit vasoconstriction, lower blood pressure. Relax smooth muscle in baldder.

30
Q

Alpha 2 antagonist.

A

Clonidine, selective. Inhibit NA release, lowers blood pressure, anxiolytic. Used in galucoma to reduce intraocular pressure. Yohimbine - erectile dysfunction.

31
Q

Non selective alpha antagonist.

A

Phentolamine, Blocks effects of excess NA. Side effects - tachycardia, nasal congestion (due to negative feedback).

32
Q

Non selective B1 agonists.

A

Cavedilol (+A1 as well), Oxprenolol.

33
Q

Selective B2 agonist.

A

Salbutamol.

34
Q

Selective B2 antagonist.

A

Butoxamine.

35
Q

Non selective B2 antagonist.

A

Propanolol.

36
Q

Effect of B2 antagonists.

A

Worsen asthma and decrease anxiety (skeletal muscle tremor).

37
Q

Selective B3 agonist.

A

BRL 37344 .

38
Q

Non selective B3 antagonist.

A

Propanalol.

39
Q

Non selective Beta agonist.

A

Isoprenaline.

40
Q

Summary.

A