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MedChem II - stack 1

Catecholaminergic drugs part 1

Drug nameDescription
Vinca alcaloids (e.g. Vincristine), paclitaxel, colchicine Block axonal transport of catecholamine NT's
Local anesthetics Inhibit catecholaminergic neurotransmission
alpha-Methyl p-Tyrosine (Metyrosine, Demser (R)) competitive inhibitor of tyrosine hydroxylase, treats pheochromacytoma
alpha-Methyldopa (Aldomet) Inhibitor of L-aromatic amino acid decarboxylase, resulting product is a false transmitter, has agonist activity at alpha2 receptors, and thus antihypertensive activity
Disulfuram (Antabuse) Inhibits acetaldehyde dehydrogenase, chelates copper cofactor in dopamine beta-hydroxylase, therefore can cause hypotension
Reserpine and other Rauwolfia alkaloids Inhibit transport of dopamine and norepinephrine into the storage vesicles, may also affect storage of serotonin
Desperidine Inhibits catecholamine storage
Guanethidine monosulfate (Ismelin Sulfate) Inhibits catecholamine storage and prevents NT release, treats moderate to severe hypertension and renal hypertension
Guanadrel Sulfate (Hylorel) Inhibits catecholamine storage, acts as a false NT, and prevents NT release, antihypertensive
Bretylium tosylate (Bretychol) Inhibits catecholamine storage and prevents NT release, originally used as antihypertensive, now discontinued
Epinephrine (Primatine Mist, Bronkaid Mist), also HCl (Adrenalin) and Borate (Epinal) Direct alpha and beta receptor agonist, treat bronchospasms, hypersensitivity reactions, prolong action of local anesthetics, restore cardiac rhythm during cardiac arrest
Norepinephrine bitartrate (Levophed) Potent alpha agonist, little action on beta-2 receptors, used in treatment of some shock syndromes
Dipiverin hydrochloride (Propine) Direct alpha and beta agonist, prodrug, used to treat open-angle glaucoma
Dobutamine hydrochloride (Dobutrex) Direct alpha and beta agonist, has complex pharmacology, used clinically for cardiac stimulation
Phenylephrine hydrochloride (Neosynephrine) Direct alpha agonist, used as a nasal decongestant and mydriatic (pupil dilation)
Metaraminol bitartrate (Aramine) Direct alpha agonist, also indirect actions, treats hypotension
Methoxamine hydrochloride (Vasoxyl) Direct alpha agonist, treats hypotension
Midorine hydrochloride (Proamatine) Direct alpha-1 agonist, treats hypotension
Imidazolines (Xylometazoline, Oxymetazoline HCl, Naphazoline HCl, Tetrahydrozoline HCl) Direct alpha-1 agonists, used as nasal and ocular decongestants, OTC
Clonidine (Catapres) Centrally acting alpha-2 agonist, treats hypertension
Guanabenz Acetate (Wytensin) Guanfacine Hydrochloride (Tenex) Analogues of clonidine, centrally acting alpha-2 agonists, treat hypertension, guanfacine-ADHD (off-label use)
Tizanidine Hydrochloride (Zanaflex) Centrally acting alpha-2 agonist, used for muscle spasticity
Apraclonidine (Iodipine) Alpha-2 agonist, reduces intraocular pressure
Brimonidine (Alphagan) Analogue of apraclonidine, more selective for alpha-2 receptors, reduces intraocular pressure, can cause systemic side effects
Isoproterenol HCl (Isuprel) Isoproterenol sulfate (Medihaler-Iso) Beta agonist, bronchodilator
Bitolerol mesylate (Ronalate) - metabolized to Colterol Beta agonist, slight beta-2 selectivity, bronchodilator
Ethylnorepinephrine (Bronkephrin) Beta agonist, little alpha agonist activity, bronchodilator
Isoetharine HCl (Arm-a-Med) Beta agonist, more beta-2 activity, very little alpha activity, bronchodilator
Albuterol and Albuterol Sulfate (Proventil, Ventolin, etc.) Beta-2 agonist, bronchodilator
Levalbuterol (Xopenex) (R)-albuterol isomer, therapeautically active agent, beta-2 agonist, bronchodilator
Pirbuterol acetate (Maxair) Beta-2 agonist, bronchodilator
Salmeterol xinafoate (Serevent) Long-acting beta-2 agonist, used for long term management of bronchospasm
Formoterol fumarate (Foradil) Long-acting beta-2 agonist, treats asthma, COPD, chronic bronchitis, and emphysema
Ritoridine HCl (Yutopar) Beta-2 agonist, used to inhibit uterine contractions in preterm labor
Pseudoephedrine Indirect acting adrenergic agonist, threo racemate of ephedrine
Dextroamphetamine sulfate (Dexedrine) Indirect adrenergic agonist, readily crosses the blood-brain barrier, treats obesity and narcolepsy
Methamphetamine HCl (Desoxyn) Indirect adrenergic agonist, previously used in treatment of ADD
Created by: 100000197460889