test 5 part 2 Flashcards
Adrenergic Antagonists
▪ Smypatholytics ▪ Adrenoreceptor antagonists ▪ Adrenergic blocking agents ▪ These drugs block “fight or flight” response –α Blockers –β Blockers
α Blockers
- profoundly affect BP
- blocks the binding of the ligand to the receptor
- end up with vessel dilation
- causes reflex tachycardia
- baroreceptors respond to decrease in BP so parasympathetic output decreases and sympathetic outflow increases
types of α Blockers
▪ Non Selective α Blockers
▪ Selective α1 Blockers
▪ Selective α2 Blockers
what does α1 do
– Increased vascular tone
what does α2 do
– Control release of norepinephrine
– Inhibitory autoreceptors
Phenoxybenzamine (Dibenzyline) uses
- Pheochromocytoma which is a tumor in the adrenal gland which causes too much catecholomine release (body has higher levels of epi and NE => sympathetic stimulation
- phenoxybenzamine blocks all of the receptors that the catecholomines are acting at
Phentolamine (Regitine) uses
– Short term treatment of pheochromocytoma
– Locally to prevent dermal necrosis when NE given peripherally
– Given locally post NE extravasation
– Epinephrine reversal
Nonspecific α Blocker Side Effects
- Orthostatic hypotension (lying down you feel fine then when you stand up and get really light headed)
- Dizziness and headache
- Tachycardia
- Sexual dysfunction
Selective α1 Blockers
▪ Competitive
▪ Decrease PVR and lower BP
▪ Minimal changes in cardiac output
▪ First dose may produce orthostatic hypotension
β Adrenergic Blockers “-olol”
▪ Competitive antagonists ▪ Vary in – Selectivity – Intrinsic sympathomimetic activity – CNS effects – Vasodilatory effects – Pharmacokinetics
β Adrenergic Blockers dosing
▪ Choice depends on side effects, patient compliance and preference
▪ Dosing must be individualized due to differences in base catecholamine levels, receptor density and variable cellular responses
β Adrenergic Blockers used to treat
▪ Hypertension ▪ Angina ▪ Cardiac arrhythmias ▪ Myocardial infarction ▪ Heart failure ▪ Hyperthyroidism ▪ Glaucoma ▪ Migraine prophylaxis
Blockade of the β1 Receptors
- Decreases force of heart
- decreases HR
- Decreases renin secretion
Blockade of the β2 Receptors
- Increase airway resistance
- Increase vascular resistance
β Adrenergic Blockers types
▪ Nonselective β blockers
▪ Selective β blockers
▪ Antagonists and partial agonists
▪ β and α blockers