Adrenergic agents Flashcards
Alpha 1 receptors
Eyes, BV, Urinary bladder, Nerve ends, Pancreas
α1 Eyes
m. Dilatator p. Contraction - mydriasis
α1 Blood vessels
skin, visceral
Arterioles
Venules
Contraction - ↑diastol.pressure,↑heart afterload
Contraction - ↑heart preload
α1 Urinary bladder
Sphincters ↑ Muscular tone
α2 Nerve ends
autoreceptors
Presynaptic pole ↓ NE release adn synthesis
α2 Pancreas
Beta cells ↓ Secretion of insulin
ß1 Eyes
Ciliar epithelium ↑ Secretion of intraocular fluid
ß1>ß2
Heart
SA node AV node Atria/ventricules His-Purkinje fibers ↑ Heart rate- «+» chronotropic e. ↑ Conduction velocity - «+» dromotropic e.; ↑Automatism ↑Contractility- «+» inotropic e. ↑Automatism
ß2 Blood vessels
(except skin, mucosa,
cerebral b/v)
Arterioles Venules Relaxation- ↓diastol.pressure (skeletal mm.), ↓heart afterload ↓heart preload
ß2 Lungs Bronchioles
↓ Muscle tone
α1,ß2 Liver
↑glycogenolysis ↑glyconeogenesis
ß2
Pancreas
Beta cells ↑ Secretion of insulin
ß2, ß3 Urinary
bladder
m.Detrusor ↓Muscle tone
ß1 Kidney
↑Release of renin
ß2 Uterus
Myometrium ↓ Muscle tone
ß2 Skeletal
muscles
↑ Muscle tone
↑ glycogenolysis,
↑K uptake in cells
EPINEPHRINE
Vasoconstrictive / vasodilatory, cardiotonic
(«+» inotropic effect), «+» Chrono-,
dromotropic effect, bronchodilatory,
mydriatic action
Receptor affinity low doses B1 & B2
high doses A1, B1 & B2
=>Anaphylactic shock
=>Asystolia
=>Topically - in combination with local anesthetics
i.m, i/v
NOREPINEPHRINE
Vasoconstrictive, cardiotonic («+» inotropic effect), mydriatic effect, Reflector bradycardia
Receptor affinity A1,A2 & B1
Norepinephrine doesn’t cause bronchodilation but causes increase myocardial oxygen demand
=>Acute hypotension - collapse SBP < 70 mm Hg
PHENYLEPHRINE
α1 adrenomimetic agents
Local action vasoconstrictors - nasal decongestants
Systemic vasoconstrictive effect → hypertensive effect (↑ BP), Causes reflector (indirect effect) «-» chronotropic effect Mydriatic effect
=> Acute rhinnitis, nose bleeding
=>Acute hypotension
=>Paroxysmal ventricular tahycardia
CLONIDINE
α2 adrenomimetic agents
- hypotensive effects (vasomotor center) of central action
Stimulation of central postsynaptic α2 receptor…↓SANS impulsation…Peripheral vasodilatation
In vasculature peripheral presynaptic autoreceptor and
postsynaptic α2 stimulation
Bradycardizing effect
Rebound effect - BP↑
- Regulates brain subcortical activity.
↓ pain impulse transmission in brain
=> Hypertension, hypertensive crisis
SALBUTAMOL
β2 adrenomimetic agents - Bronchodilatators
1. ↓ intracellular calcium concentration, Relaxation of nrochial smooth muscle → bronchodilation => Bronchial asthma attack 2. Tocolytic effect (inhibition of uterus contractions) =>Tocolysis
SE: tremor, tachycardia (β2 heart)
MI: reduces effects of vasoconstrictive agents
DOXAZOSINE
α1 selective blockers
- Vasodilatation of peripheral blood vessels, vein and artery
↓peripheral resistance (reduces afterload),
increases capacity of veins (reduces preload)
and ↓ BP, hypotensive effect
=>Hypertension - ↓ urethral tone and relaxes prostate muscle
↓ urination disorders
=> Symptomatic therapy of prostate
adenoma
SE: first-dose orthostatichypotension and
syncope, reflector tachycardia
BAB
1st gen
Nonselective β1, β2 adrenoblockers
PROPANOLOL
=>Coronary artery disease
=>Tachycardia, thyrotoxicosis, prevention of migraine attacks
=> Atrial fibrilation (Class II antiarrhythmics)
SE: bradycardia, AV block, risk of bronchial obstruction,
sexual dysfunction, Raynaud syndrome
MI: Due to non-selective action, P may affect the effects of adrenopositive agents
For diabetic patients its better to use cardioselective BAB as non selective can mask effects of insulin overdose
Sudden stopping of drug can cause rebound effect!
TIMOLOL
eye drops
↓ intraocular fluid secretion in the ciliary body reduces IO pressure
=>Glaucoma
BAB
2nd gen
Cardioselective β1 adrenoblockers
METOPROLOL
Bisoprolol highly selective β1 => CAD =>Hypertension =>Atrial fibrilation (Class II antiarrhythmics) =>CHF (chronic heart failure) =>Prophylaxis of migraine attacks
Cardioselectivity β1…
- less impact on b / v smooth muscle, bronchi, uterus and
- electrolyte balance (risk of hyperkalemia is lower)
- safer for patients with asthma, * DM and Raynaud syndrome.
- β2 blockade reduces insulin secretion and glycogenolysis
BAB
3rd gen
α1, β1, β2 adrenoblockers
CARVEDILOL
Cardiodepressant + reduces peripheral vascular resistance
+ antioxidant properties
(cardioprotection, inhibits lipid peroxidation)
=>Chronic heart failure
=>CAD
=>Hypertension
RAYNAUD SYNDROME
BAB causes peripheral vasoconstriction…limb freezing.
Raynaud syndrome is a group of peripheral circulatory disorders characterized by episodic stenosis of limb arteries and arterioles.
Usually provoked by cold or stress.
Manifested as sudden paleness or cyanosis of the fingers and toes,
including the earlobe and nose