Autonomic Pharm 1
Terms
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- It blocks the enzyme that converts tyrosine to dopa (tyrosine hydroxylase). Over time it decreases the amount of tranmitter stored in the nerve. It is used extensively in management of pheochromocytoma.
- Alpha-methyl-tyrosine
- It blocks the vesicular pump into storage vesicles and eventually depletes a nerve of its transmitter. No synthesis or storage of Norepinephrine. Effective in management of high blood pressure and a sedative because it reduces storage of central amines.
- Reserpine
- This interferes with coupling of action potential to vesicle docking. It does not have an effect on parasympathetic nerves. Potent and orally effective antihypertensive.
- guanethidine
- An alpha receptor antagonist that doesn't have much of an effect on pre-synaptic receptors.
- Prazosin
- A beta blocker, blocks interaction of Ne with receptor. A cardioprotective agent that prevents arrhymia and helps treat angina.
- Propanolol
- A COMT inhibitor, used with schizophrenia.
- Pyrogallol
- An MAO inhibitor that inhibits breakdown of Ne and Epi.
- Pargyline
- This blocks the neuronal uptake pump and increases norepinephrine in the synapse. Also has some effects on the peripheral nervous system - like hypertension and arrythmia.
- Cocaine
- This has selectivity for pre-synaptic Alpha-2 receptors. It reduces the amount of transmitter in hte synapse by acting very much like Norepinephrine feedback. It is a good anti-hypertensive agent. Most of its action is central, can be used as a sedative
- Clonidine
- This compound blocks alpha receptors, but not beta receptors.
- Phenoxybenzamine (PBZ)
- This compound blocks beta responses, but not alpha
- Dichloroisoproterenol (DCI)
- Agent acts on A1, A2, B1, B2
- Epinephrine
- Agent acts on A1, A2, B1
-
Norepinephrine
(does not act on B2) - These agents act only on A1 receptors
- Phenylephrine, methoxamine
- This agent acts on A2 receptors only
- Clonidine
- This agent acts on B1 and B2 receptors
- Isoproterenol
- This agent acts on B1 receptors
- Dobutamine
- These agents act on B2 receptors
- Terbutaline, albuterol, metaproterenol
- This is a mixed action sympathomimetic
- Ephedrine
- This is an indirectly acting sympathomimetic agent
- Amphetamine and Tyramine
- These agents are antagonists to A1 and A2 receptors
- Phenoxybenzamine and phentolamine
- This antagonizes A1 receptors
- Prazosin
- This antagonizes A2 receptors
- Yohimbine
- These agents antagonize B1 and B2 receptors
- Propranolol, timolol, pindolol, nadolol
- These agents are antagonists to B1 receptors
- Metoprolol, atenolol, alprenolol
- This agent is an antagonist to A1 and beta receptors
- Labetalol
- This drug is not selective for alpha receptors, but is an agonist of both beta receptors, equally
- Isoproterenol
- This is the only non-selective agonist for adrenal receptors
- Epinephrine
- This adrenergic agonist is selective for B1 receptors
- Dobutamine
- These drugs works well as A2 agonists
- Alpha methyl dopa and Clonidine
- Trade name Levophed
- Levarterenol = Norepinephrine
- Trade name Adrenalin
- Epinephrine
- Trade name Isuprel
- Isoproterenol
- Main type of receptor in skin
- A1
- Main type of receptor in viscera
- A1 (some B2, but way more alpha than beta so isoproterenol doesn't have much effect)
- Main type of receptor in Skeletal muscle
- B2 - NE causes constriction, isoproterenol causes dilation. Epinephrine effects are dose dependent, biologic levels dilate, high concentrations constrict
- Main type of receptor in pulmonary
- A1
- Type of receptors in coronary arteries
- Beta, but mainly they are under autoregualtion
- Decreased PVR, increased systolic BP
- Isoproterenol
- increased PVR, increased systolic, diastolic, and mean BP, decreased HR, increased CO
- Norepinephrine
- Decreased PVR and diastolic, increased systolic, but only under therapeutic levels. HR increases.
- Epinephrine
- Muscarinic antagonist
- Atropine, blocks PNS effects
- Main receptor on bronchial smooth muscle
- B2 - iso and epi work well to dilate
- Main receptor in GI
- B2, inhibits tone and motility
- Main receptor in Iris
- A1, NE and Epi cause mydriasis
- This catecholamine can only be administered via IV
- Norepinephrine
- This drug has a very limited therapeutic value but can be used for hypotension if there's good CO and tissue perfusion.
- Norepinephrine
- This drug is used a lot and is good with anaphylactic shock and to prolong the action of local anesthetics. Also helps with cardiac arrest and open angle glaucoma
- Epinephrine
- This drug is used in cases of bronchospasm, cardiac arrest, and heart block
- Isoproterenol
- The vasoconstricting effects of this drug helps to keep local anesthetic in the system longer
- Epinephrine
- Why doesn't NE cause tremor and weakness like Isoproterenol and Epinephrine?
- Because it doesn't stimulate B2. These drugs all cause fear, anxiety, and restlessness. Also palpitations.
- Epinephrine, NE, and isoproterenol should be used with caution in what kinds of patients?
- Those with hyperthyroidism (thyroid makes B2 receptors more sensitive), hypertension, and angina pectoris.
- Anesthetics and catecholamines do what to the heart?
- Sensitize myocardium and create arrythmia
- What are two serious side effects of catecholamines?
- Cerebral hemorrhage, arrhythmia (particularly with halogenated anesthetics)