Autonomic nervous system receptors (adrenergic and cholinergic drugs)

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82 terms · Pharmacology lecture 3

Alpha 1 receptor sympathetic effects

Contraction of smooth muscle, exocrine gland secretion, and neuronal excitation

Alpha 2 receptor sympathetic effects

Inhibition of Nor adrenaline release Decreased secretion of aqueous humour and insulin

Beta 1 receptor sympathetic effects

Mainly increased HR and contraction. Increased renin secretion

Beta 2 receptor sympathetic effects

Glycogenolysis, smooth muscle relaxation Uptake of potassium into skeletal muscle

Beta 3 receptor sympathetic effects

Lipolysis in adipose tissue

Muscarinic M1 receptor parasympathetic effects

Modulation of neurotransmission (neural)

Muscarinic M2 receptor parasympathetic effects

Slowing of HR and contraction (maintains homeostasis in conjunction with Beta 1)

Muscarinic 3 receptor parasympathetic effects

Contraction of smooth muscles and stimulation of glandular secretions (saliva) and Vascular smooth muscle dilation = vasodilation

Nicotinic Nm receptor parasympathetic effects

Contraction of muscles

Nicotinic Nn receptor parasympathetic effects

Excitation of postganglionic neurons

Effects of Nor adrenaline on Beta 1

>HR
>contractility (<cardiac efficiency)
> risk of arrhythmia

Effects of Nor adrenaline on Alpha 1

Vasoconstriction of blood vessels

Effects of Nor adrenaline on Alpha 2

Vasoconstriction of blood vessels
< neurotransmitter release

Is adrenaline an adrenocepter agonist or antagonist

direct acting adrenoceptor agonist

Effects of Nor adrenaline on Beta 2

Vasodilation
Bronchodilation
Mobilize energy stores

Is dobutamine an adrenoceptor agonist or antagonist

direct acting adrenoceptor agonist

What is the mode of action of Dobutamine

Stimulates Beta 1 and Beta 2 receptors

What is the mode of action of Adrenaline

Stimulates Alpha 1 & 2 and Beta 1 & 2 receptors

What is the pharmacological effect of Dobutamine

> in HR and > in contractility (Beta 1)
Vasodilation (Beta 2)

What is the pharmacological effect of Adrenaline

Vasoconstriction > BP (α1),
cardiac stimulation, >HR and force of contraction (β1),
bronchodilation (β2)

Side effects of dobutamine

Arrhythmias

Side effects of adrenaline

Hypertension and arrhythmias

Are salbutamol and salmeterol adrenoceptor agonists or antagonists

direct acting adrenoceptor agonists

What is the mode of action of salbutamol and salmeterol

bind to beta 2 receptors

What is the pharmacological effect of salbutamol and salmeterol

Bronchodilation due to smooth muscle relaxation

Side effects of salbutamol and salmeterol

tachycardia and arrythmias

What is phenylephrine agonist or antagonist

Direct acting adrenoceptor agonist

What is phenylephrine mode of action

Binds to alpha 1 receptors

What is the pharmacological effect of phenylephrine

vasoconstriction leading to > in BP

side effects of phenylephrine

bradycardia
hypertension

What is amphetamine direct or indirect

Indirect acting adrenoceptor agonist

What is the mode of action of an amphetamine

Causes an increase in the release of noradrenaline from the storage vesicles

Side effects of amphetamines

Hypertension
tachycardia
dependance

what is the pharmacological effect of amphetamines

CNS stimulant increases brain activity

what is cocaine direct or indirect

Indirect acting adrenoceptor agonist

What is the mode of action of cocaine

Inhibits uptake of noradrenalin

Side effects of cocaine

Hypertension
cardiac damage
necrosis of nasal mucosa

what is the pharmacological effect of cocaine

vasoconstriction due to increase in noradrenalin levels

What is pseudoephedrine

A mixed acting adrenoceptor agonist

what is psuedoephedrine mode of action

Causes release of nor adrenaline from storage vesicles in the presynaptic neuron.

Pharmacological effect of pseudoephedrine

Vasoconstriction due to increased NA being availablet o bind to the alpha 1 receptors of blood vessels

What is ephedrine

a mixed acting adrenoreceptor agonist

what is ephedrines mode of action

Causes more nor adrenaline to be released from the storage vesicles

Pharmacological effects of ephedrines

Vasoconstriction due to increased NA being available to bind to the alpha 1 receptors.

Side effects of ephedrine and pseudoephedrine

hypertension
tachycardia
insomnia and dependance

What is prazosin

adrenergic antagonist (alpha blocker)

What is the mode of action of prazosin

alpha 1 receptor blocker

pharmacological effects of prazosin

decreased vascular resistance due to vasodilation
drop in BP relax bladder and prostate

side effects of prazosin

orthostatic hypotension
Nasal congestion
urinary urgency

what is phentolamine

adrenergic antagonist ( alpha blocker)

what is the mode of action of phentolamine

blocks alpha 1 and 2 receptors

what are the pharmacological effects of phentolamine

decreased vascular resistance due to vasodilation and resultant drop in BP

what are the side effects of phentolamine

orthostatic hypotension
tachycardia
nasal congestion

What is atenolol

adrenergic antagonist (beta blocker)

What is the mode of action of atenolol

blocks the beta 1 receptor

what are the pharmacological effects of atenolol

reduces cardiac rate and output
reduces Av node conduction
reduces O2 demand
reduces BP

What are the side effects of atenolol

cardiac failure
hypoglycemia
bronchoconstriction

What is propanolol

An adrenergic antagonist (beta blocker)

what is the mode of action of propanolol

blocks beta 1 and 2 receptors

what is the pharmacological effect of propanolol

reduces cardiac rate and output
reduces AV node conduction
reduces O2 demand
reduces BP

what are the side effects of propanolol

cardiac failure
bronchoconstriction
hypoglycemia

what is carvedilol

an adrenergic atagonist (alpha and beta blocker)

what is the mode of action of carvedilol

blocks beta 1 and 2 receptors and alpha 1 receptors

what is the pharmacological effect of carvedilol

In pts with hypertension vasodilation drop in HR and BP
in Pts with heart failure increase in cardiac output

side effects of carvedilol

cardiac failure
hypoglycemia
bronchoconstriction
renal failure

What are the side effects of muscarinic stimulation

diarrhoea, urination, miosis, bronchoconstriction, emesis, lacrimation and salivation.

What is nicotine

a direct acting cholinergic agonist

What receptor does nicotine act on

Nicotinic receptor

What can nicotine be used for

Smoking cessation

what is pilocarpine

A direct acting cholinergic agonist

what receptor does pilocarpine act on

M3 and nicotinic receptors

what can pilocarpine be used for

xerostomia treatment, glaucoma due to reduction of intraocular pressure

what are the 2 types of nicotinic antagonists

Non de-polarising (blocks Ach receptors: Ach can't bind so no influx of Na and no depolarisation)
Depolarising (agonists at Ach receptors)

what is an example of a non-depolarising antagonist

tubocurarine analogues

what is the use of a non-depolarising antagonist

neuromuscular blockers muscle relaxation for surgical anaesthesia Can be used for fixing mandibular fractures

What is an example of a depolarising antagonist

suxamethonium

What can suxamethonium be used for

brief procedures such as endoscopy and colonoscopy

What was the first reversible muscarinic antagonist (anticholinergic drug)

atropine

How does atropine work

blocks the effects of the vagus nerve on the heart therefore increases heart rate

What are 3 other anticholinergics

pirenzepine (M1 inhibition of gastric secretion)
hyoscine (anti emetic and antispasmodic)
ipratropium (bronchodilation)

What are the side effects of atropine OD

Dry mouth, decreased sweating, increased HR,blurred vision, tachycardia, palpitations, urinary retention, restlesness, fatigue, rapid weak pulse, ataxia, hallucinations, delerium and coma

What is most significant side effect for dentistry of anticholinergics

xerostomia

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