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Notes for Pharmacology (for understanding of RM lecture)

There are a few types of receptors


Agonist
Reversible
antagonist
Cholinergic
Acetylcholine
a) Mascarinic
Mascarin
Atropine
b) Nicotinic
Nicotine
d-tubocurarine
1
Noradrenaline
Prazosin
B1
Noradrenaline
Propranolol
B2
Isoprenaline,
salbutamol
Opioid
Morphine
Naloxone

Irreversible
antagonist

Phenoxybenzamine

**Noradrenaline = norepinephrine. Adrenaline = epinephrine


First we can look back to our term one lecture on the Autonomic Nervous System

Cholinergic means "having to do with acetylcholine". The neurotransmitter


acetylcholine is released from the terminals of all preganglionic neurons in both the
sympathetic (orange) and the parasympathetic (blue) divisions of the ANS. There are
two categories of cholinergic receptors -- nicotinic and muscarinic.
Nicotinic Receptors

Acetylcholine is the neurotransmitter released from both the preganglionic and the
postganglionic neurons of the parasympathetic division.
Nicotine injected into laboratory animals causes some organs to respond as if
acetycholine had been injected. Thus, the receptors to which both acetylcholine and
nicotine can attach are called "nicotinic."
Muscarinic Receptors
Muscarine, derived from the mushroom Amanita muscaria, injected into laboratory
animals causes some organs to respond as if acetylcholine had been injected. Thus,
the receptors to which both acetylcholine and muscarine can attach are called
"muscarinic."
Atropine, an antagonist for muscarinic ACh receptors, lowers
the parasympathetic activity of muscles and glands in the parasympathetic nervous
system.
Tubocurarine can cause paralysis. Its an antagonist for nicotinic receptors, meaning it
blocks the receptor site from Ach.
Nicotine and mascarin causes the parasympathetic division to be triggered heart
beat slower, more digestion etc. (rest and digest)
Receptor
Beta 1

Location
Heart

Beta 2

Vascular and non vascular


smooth muscle

Alpha 1

Blood vessels

Effect
increases in contractile
force and heart rate
vascular and nonvascular
smooth muscle relaxation,
treat asthma
increases vascular smooth
muscle contraction,
producing increase in
blood pressure

Alpha 1 receptors
Activation of alpha 1 receptors increases vascular smooth muscle contraction,
producing increases in blood presure. These receptors also influence activity of
genitourinary smooth muscle.

Effects of alpha 1 receptor activation on different tissues and systems:


Vascular smooth muscle. Activation of vascular smooth muscle receptors
causes vasoconstriction, leading to an increase in peripheral resistance and in
blood pressure. Alpha 1 antagonists are used in the treatment of hypertension
because of their properties as peripheral vasodilators.
Mydriasis. Mydriasis is mediated by both alpha 1 and 2 activation.
Genitourinary tract smooth muscle. Alpha 1A receptors are located at the
external sphincter of the bladder. Blockade of alpha 1A receptors decreases
tone in the smooth muscle of the bladder neck and prostate, thus improving
urinary flow. Tamsulosine is used for the treatment of benign prostatic
hyperplasia because of its ability to selectively block alpha 1A receptors.
Effect of Beta 1 Receptor Activation on the Heart: Activation of the beta 1 receptor
leads to increases in contractile force and heart rate. Drugs that activate the
beta1 receptor can be used in heart failure to improve the contractile state of the failing
heart. Drugs that activate the beta1 receptor also increase heart rate. Indeed, excess
stimulation the beta 1 receptor can induce significant increases in heart rate
and arrhythmias. Arrhythmias are a major concern with drugs such as epinephrine that
can be absorbed systemically after intra-oral injection.

Effect of Beta 2 Receptor Activation on Smooth Muscle: Activation of the beta


2 receptor leads to vascular and nonvascular smooth muscle relaxation. Drugs that
activate the beta2 receptor can be used to treat as asthma (by relaxing airway smooth
muscle) and premature labor (by relaxing uterine smooth muscle).
Morphine is acts on CNS to decrease the feeling of pain/ analgesic
Some of the drugs mentioned and their functions:
Drug
Function
Diazepam, pentobarbitone, barbiturate
CNS depressant
Warfarin
Anticoagulant/blood-thinner

Made by Leng Wei


No guarantee that all info are correct, so dont trust these things completely, but Ive
tried my best to get the most accurate info that I can find.
Do let me know if theres anything wrong

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