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44 Cards in this Set

  • Front
  • Back

Adrenergic drugs - agonists




Main types

Alpha 1, Alpha 2


Beta 1, Beta 2


Non selective Alpha/Beta


Non selective Beta


Non selective Alpha

Alpha 1 Agonists
Drugs

Phenylephrine


Xylometazoline

Alpha 1 drugs


-Main physiological effects


- Uses

Effects:


1) Smooth muscle contraction


2) Vasoconstriction


-> increase peripheral resistance


-> Increase AP


Uses:


Nasal decongestion

Phenylephrine


Actions, uses, unwanted effects, indications

Actions: alpha 1 agonist


Uses: Nasal decongestion


Unwanted effects: hypertension, bradycardia


Indication: Used intranasally

Beta 1 Agonists


Drugs

Dobutamine (B-1 selective)


Isoprenaline (B non selective)
Adrenaline and Noradrenaline (A-B non selective)


Dopamine

Beta 1 agonists


Main physiological effects


Main uses:

effects:


1) increase contractile force of the heart (inotropic)


2) Increase heart rate (chronotropic)


can lead to arrythmia


Uses: Cardiogenic shock

Dobutamine


Actions, uses, unwanted effects, indications

Actions: B-1 agonist


Uses: Cardiogenic shock


Unwanted effects: dysrhytmias


Indications: given by IV



Isoprenaline


Actions, uses, unwanted effects, indications

Actions: B agonist (vasodilation)


Uses: Asthma - relaxes the smooth muscles of the lungs,


Unwanted effects: Tachycardia, dysrhytmias


Indication: replaced by salbutamol for asthma



Epinephrine and Norepinehprine


Actions, uses, unwanted effects, indications

Actions: A/B agonist


Uses: Asthma, anaphylactic shock, cardiac arrest


Unwanted effects: Hypertension, vasoconstriction, tachycardia, dysrhytmias.


Indication: subcutaneously, poorly absorbed by mouth.


Noradrenaline is mainly an A agonist, and causes vasoconstriction

B-2 agonists


Drugs

Salbutamol


Ephedrine



B-2 agonists


Main physiological effects


Main uses

1) Vascular and smooth muscle relaxation


used for asthma treatment and premature labor.

Salbutamol


Actions, uses, unwanted effects, indications

Actions: B-2 agonist


Uses: Asthma, premature labour


Unwanted effects: Tachycardia, dysrhytmias, tremor, peripheral vasodilation

A-2 drugs

Methyldopa


Clonidine

Clonidine


Actions, uses, unwanted effects, indications

Action: A-2 partial agonist


Uses: hypertension, migraine


Unwanted effects: weight gain, drowsiness, hypotension, rebound hypertension.


Indications: Oral administration

Amphetamine


Actions, uses, unwanted effects, indications

Actions: NA release, CNS stimulant


uses: narcolepsy, ADHD


Unwanted effects: hypertension, tachycardia, insomnia, dependance, can be fatal in OD.


Indications: do not take if MAO inhibitors were given.

Ephedrine


Actions, uses, unwanted effects, indications

Actions: Na release, weak CNS stimulant


Uses: Nasal decongestion


Unwanted effects: like amphetamine but less.


Indications: do not take if MAO inhibitors were given.

Adrenergic drugs


Main types

Beta blockers


Alpha blockers



Beta blockers drugs

Propanolol, Timolol, atenolol, metoprolol, labetalol

Propranolol


Actions, uses, unwanted effects, indications

Actions: B antagonist (non selective)


Uses: Angina, hypertension, dysrythmias, tremor, glaucoma


Unwanted effects: Bronchoconstriction, cardiac failure, fatigue, depression, hypoglycaemia.


Indication: Absorbed orally

Metoprolol


Actions, uses, unwanted effects, indications

Same as propranolol, but it's a B -1 antagonist, and has a lesser risk of bronchoconstriction.

A- blockers drugs

Prazosine A-1


Doxazosine A-1


Tamulosine


Yohimbine A-2


Phentolamine A non selective

A blocker drugs


Main effects

A1 antagonists will work like B-2 agonists. Smooth muscle relaxation, vasodilation, fall in arterial pressure.

Prazosine and Doxazosine


Actions, uses, unwanted effects, indications

Action: A-1 antagonist


Uses: Hypertension


Unwanted effects: tachycardia, nasal congestion, impotence, postural hypotension


Indications: absorbed orally.

Tamulosine

A1a selective, acts mainly on the urogenital tract.

Yohimbine


Actions, uses, unwanted effects, indications

Action: A -2 antagonist


Uses: not used clinically


Unwanted effects: hypertension


Indication: absorbed orally



Phentolamine


Actions, uses, unwanted effects, indications

Action: A antagonist


Uses: rarely used


Unwanted effects: Postural hypotension, tachycardia, nasal congestion


Indication: IV administration

Cholinergic agonists


Drugs

Acetylcholine


Nicotine


Pilocarpine


Carbachol


Betanechol

Acetylcholine


transmission

1- AP depolarizes synpatic knob


2- Ca2+ enters cytoplasm, Ach released from synaptic vesicle


3- Ach binds to nicotinic receptor(depolarization)


4- Ach broken down from AchE (ms)


5- Synpatic knob reabsorbs choline


6- Ach reformed in the synaptic vesicle

Acetylcholine pharmacological blocks

Hemicholinium: inhibits choline uptake


Botolintoxin: inhibits Ach release


Suxamethonium: block postsynaptic receptors

Carbachol

M receptor agonist


Induceses miosis

Pilocarpine


Description

M3 agonist, used as eye drops to treat glaucoma: reduces intra-ocular pressure, causes the pupils to constrict and to drain the excess aqueous humour.

Nicotine

Slows down heart rate


Vasodilation


lowers arterial blood pressure


increases GI motility (smooth muscles contraction)


Increase glandular/salivary secretions

Muscarinic antagonists


drugs

Atropine


Pirenzepine


Hyoscine (Scopolamine)


Tropicalamide


Oxybutinin


Ipratropium (tiotropium)

Atropine

- Lowers secretions


- Increases heart rate


- dilates pupiles


- Decreases GI motility


- Decreases glandular secretions


- smooth muscle relaxation


May cause hyperactivity and delirium

Hyoscine (scopolamine)

acts mostly like atropine, but its a CNS depressant

Pirenzepine

M1 selectivity


inhibits gastric secretion


used for peptic ulcers

Tropicamide

similar to atropine


may raise intraocular pressure


dilation of the pupils and cycloplegia.

Ipratropium

similar to atropin but doesnt inhibit mucocilliary secretions from bronchi.


used to treat bronchitis and asthma.

Neuro muscular blocking drugs


Main principles

presynaptically inhibit Ach release/synthesis.


inihibit post synaptic Ach action.

Neuro muscular blocking drugs

Tubocurarine


Pancuronium


Vecuronium


Atracurium


Mivacurium


Suxamethonium ( the only depolazing drug, i.e causing persistant depolarization)



Tubocurarine


Onset, duration, main side effects, indications

Onset: slow,


Duration: long


Side effects: hypotension, bronchoconstriction (related to histamine release).


histamine = vasodilation = lowers arterial blood pressure. too much histamine not good.

Suxamethonium


Onset, duration, main side effects, indications

Onset: fast


Duration: short


Side effects: Bradycardia, dysrythmias, hyperthermia, raised intraocular pressure


Indication: Plasma cholinesterase metabolises the drug very fast, slower in pts with liver disease.

Anticholinesterase drugs


Main effects:

enhancement of Ach activity in postganglionic synapses.


Increases secretions, increased persitlatic activity, pupillary constriction.


More depolarizations at the postsynaptic neuron.



Anticholinesterase drugs


Main side effects

CNS - hallucinations


GI tract - hypermotility


Bradycardia