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| Drug Name | Category | Mechanism, Indications, Adverse Effects, Unique Properties |
| Dopamine | Adrenergic Agonist, Direct | Important in maintenance of renal blood flow. Dopamine receptors are found in kidneys. Has Epi-like activity at high doses. Can be used in cardiogenic shock. Can cause nausea and vomiting |
| Oxymetolazine | Adrenergic Agonist, Direct
alpha1, alpha2 |
Topical nasal decongestant (via action on alpha1 receptors). In high doses, can paradoxically produce hypotension, probably via alpha2 receptors. |
| Xylometolazine | Adrenergic Agonist, Direct
alpha1, alpha2 |
Topical nasal decongestant. |
| Norepinephrine | Adrenergic Agonist, Direct
alpha1, alpha2, beta1 |
Increase b.p. ------> reflex bradycardia.. If reflexes are blocked by Hexamethonium, then you see a direct tachycardia. |
| Methoxamine | Adrenergic Agonist, Direct
alpha1-selective |
Used to maintain blood pressure during anesthesia. Produces fewer arrhythmias than other drugs. |
| Naphazoline | Adrenergic Agonist, Direct
alpha1-selective |
Used to induce mydriasis before ophthalmic exam. |
| Phenylephrine | Adrenergic Agonist, Direct
alpha1-selective |
Used topically as a nasal decongestant (restrict blood flow to nose), and to
induce mydriasis for ophthalmic exam.
Not a catechol, and not broken down by COMT, thus it has longer half-life (20 minutes) then catecholamines. alpha-Agonist ------> increase b.p. ------> reflex bradycardia. |
| Clonidine | Adrenergic Agonist, Direct
alpha2-selective |
Prototypical alpha2-Agonist ------> inhibit sympathetics (and some
parasympathetics). It is an indirect adrenergic antagonist, as it decreases
sympathetic outflow.
Initially it produces a transient hypertension (via alpha2 vascular receptors), followed by prolonged hypotension. |
| Guanabenz | Adrenergic Agonist, Direct
alpha2-selective |
It is an indirect adrenergic antagonist, as it decreases sympathetic outflow. |
| Guanfacine | Adrenergic Agonist, Direct
alpha2-selective |
It is an indirect adrenergic antagonist, as it decreases sympathetic outflow. |
| Methyldopa | Adrenergic Agonist, Direct
alpha2-selective |
alpha-methyl-NE is the active form, converted by DOPA-decarboxylase and Dopamine-beta-Hydroxylase into the active form. alpha-methyl-NE slowly replaces endogenous NE in pre-synaptic neurons, to induce the inhibitory physiologic effect of decreasing sympathetic outflow. |
| Isoproterenol | Adrenergic Agonist, Direct
beta-selective (beta1, beta2) |
Given sublingually or by inhalation. Produces hypotension (beta2), tachycardia (beta1), and higher CO. Rapidly metabolized by COMT in liver. |
| Albuterol | Adrenergic Agonist, Direct
beta2-selective |
Bronchodilator |
| Bitoterol | Adrenergic Agonist, Direct
beta2-selective |
Bronchodilator. Prodrug is hydrolyzed in the lung by esterases to its active form, colterol. |
| Isoethanine | Adrenergic Agonist, Direct
beta2-selective |
Bronchodilator |
| Metaproterenol | Adrenergic Agonist, Direct
beta2-selective |
Bronchodilator |
| Pirbuterol | Adrenergic Agonist, Direct
beta2-selective |
Bronchodilator |
| Ritodrine | Adrenergic Agonist, Direct
beta2-selective |
Used to relax the uterus during labor. |
| Terbutaline | Adrenergic Agonist, Direct
beta2-selective |
Bronchodilator |
| Epinephrine | Adrenergic Agonist, Direct
Non-selective (alpha1, alpha2, beta1, beta2) |
Increase b.p. (alpha1) and direct tachycardia (beta1). |
| Dobutamine | Adrenergic Agonist, Direct
"Cardioselective" (B1) |
Displays some alpha1 effects. Used for cardiogenic shock and CHF.
Increases the inotropic state, with little effect on heart-rate or TPR (because it is modulated by alpha1 agonist). |
| Ephedrine | Adrenergic Agonist, Indirect
Mixed-receptor agonist |
Taken orally, long duration of action. Used in asthma, as nasal decongestant, and sometimes as a pressor.
Has direct effects (alpha1, beta1, beta2), and indirect effects (potentiate NE release). Uptake I is required for the indirect effects. Cocaine eliminates this response. Tachyphylaxis is observed peripherally but not centrally. |
| Metaraminol | Adrenergic Agonist, Indirect
Mixed-receptor agonist |
Used for the treatment of hypotension. Overall effects similar to NE, but it
is less potent and longer acting. Because of reflex bradycardia, it actually
slightly decreases cardiac output, but increases force of contraction.
Has direct effects (alpha1, beta1, beta2), and indirect effects (potentiate NE release). Uptake I is required for the indirect effects. Cocaine eliminates this response. |
| Pseudoephedrine | Adrenergic Agonist, Indirect
Mixed-receptor agonist |
Taken orally, long duration of action. Used in asthma, as nasal decongestant, and sometimes as a pressor.
Has direct effects (alpha1, beta1, beta2), and indirect effects (potentiate NE release). Uptake I is required for the indirect effects. Cocaine eliminates this response. Tachyphylaxis is observed peripherally but not centrally. |
| Clorgyline | Adrenergic Agonist, Indirect
NE-Potentiating Agent MAO Inhibitor |
MAO-A-selective inhibitor. |
| Deprenyl | Adrenergic Agonist, Indirect
NE-Potentiating Agent MAO Inhibitor |
MAO-B-selective inhibitor. |
| Pargyline | Adrenergic Agonist, Indirect
NE-Potentiating Agent MAO Inhibitor |
Non-selective MAO inhibitor. |
| Tranylcypromine | Adrenergic Agonist, Indirect
NE-Potentiating Agent MAO Inhibitor |
Non-selective MAO inhibitor. |
| Cocaine | Adrenergic Agonist, Indirect
NE-Potentiating Agent Uptake I Inhibitor |
Blocks Uptake I (NE reuptake), thus potentiating the effects of NE. |
| Imipramine | Adrenergic Agonist, Indirect
NE-Potentiating Agent Uptake-I Inhibitor, Tri-Cyclic Antidepressant |
|
| Amitriptyline | Adrenergic Agonist, Indirect
NE-Potentiating Agent Uptake-I Inhibitor, Tri-Cyclic Antidepressant |
|
| Tyramine | Adrenergic Agonist, Indirect
NE-Releasing Agent |
Potentiates NE release in pre-synaptic neuron. Serves as a false substrate for
MAO. Uptake I of tyramine is required in order for it to work, thus it is
neutralized by Cocaine.
It is dangerous to eat tyramine (wine + cheese) in patients taking MAO-inhibitors, as it can lead to hypertensive crisis. |
| Amphetamine | Adrenergic Agonist, Indirect
NE-Releasing Agent Amphetamine |
Promotes release of NE, Dopamine, and serotonin from CNS neurons. Not a catechol, and not a substrate for MAO or COMT, thus it is long-lasting. Does not require uptake I. |
| Methamphetamine | Adrenergic Agonist, Indirect
NE-Releasing Agent Amphetamine |
Promotes release of NE from pre-synaptic neuron. More pronounced CNS effects than amphetamine. |
| Methylphenidate | Adrenergic Agonist, Indirect
NE-Releasing Agent Amphetamine |
Similar to Methamphetamine, with abuse potential. |
| Pemoline | Adrenergic Agonist, Indirect
NE-Releasing Agent Amphetamine |
Similar to Methamphetamine, with abuse potential. |
| Phenmetrazine | Adrenergic Agonist, Indirect
NE-Releasing Agent Amphetamine |
Similar to Methamphetamine, with abuse potential. |
| Doxazosin | Adrenergic Antagonist
alpha-Antagonist, alpha1-Selective |
Similar to Prazosin but with longer half-life. |
| Prazosin | Adrenergic Antagonist
alpha-Antagonist, alpha1-Selective |
Has less of an effect on reflex tachycardia and renin release, because it does not block the inhibitory alpha2 receptors. It can be used to treat hypertension. |
| Terazosin | Adrenergic Antagonist
alpha-Antagonist, alpha1-Selective |
Similar to Prazosin but with longer half-life. |
| Urapidil | Adrenergic Antagonist
alpha-Antagonist, alpha1-Selective |
Has less of an effect on reflex tachycardia and renin release, because it does not block the inhibitory alpha2 receptors. It can be used to treat hypertension. |
| Labetalol | Adrenergic Antagonist
alpha-Antagonist, alpha1-Selective beta-Antagonist, non-selective |
Causes hypotension, but is accompanied by less tachycardia than other
alpha-antagonists, because it also has beta-antagonizing activity.
Local anesthetic membrane-stabilizing activity. |
| Yohimbine | Adrenergic Antagonist
alpha-Antagonist, alpha2-selective |
The only alpha2-selective antagonist there is. May be useful in autonomic insufficiency. |
| Phenoxybenzamine | Adrenergic Antagonist
alpha-Antagonist, non-selective |
Used in management of pheochromocytoma, and surgery that follows.
Irreversible binding to alpha-receptors. 14 to 48 hour duration after a single dose. Causes marked orthostatic hypotension. Causes hypotension (primary effect), reflex tachycardia, and reflex release of renin. |
| Phentolamine | Adrenergic Antagonist
alpha-Antagonist, non-selective |
Used in management of pheochromocytoma.
Blocks alpha-receptors and serotonin receptors. It is an agonist at muscarinic and histaminic receptors. Poor oral bioavailability, and short duration of action. Causes hypotension (primary effect), marked tachycardia (both due to reflex, and because NE release is increased because of alpha2 blockade), and reflex release of renin. |
| Tolazoline | Adrenergic Antagonist
alpha-Antagonist, non-selective |
Similar to Phentolamine, but less potent and more readily absorbed orally.
Causes hypotension (primary effect), reflex tachycardia, and reflex release of renin. |
| Acebutolol | Adrenergic Antagonist
beta-Antagonist, beta1-Selective |
Has partial beta-agonist activity. Local anesthetic membrane-stabilizing
activity.
Cardioselective: safer for use with asthmatics. |
| Atenolol | Adrenergic Antagonist
beta-Antagonist, beta1-Selective |
Cardioselective: safer for use with asthmatics. |
| Betaxolol | Adrenergic Antagonist
beta-Antagonist, beta1-Selective |
Decrease aqueous humour production, used to treat open-angle glaucoma. Cardioselective: safer for use with asthmatics. |
| Esmolol | Adrenergic Antagonist
beta-Antagonist, beta1-Selective |
Unusually short half-life of 10 minutes. Used in surgery, where it blocks the
reflex tachycardia and renin release that accompanies the use of vasodilators.
Cardioselective: safer for use with asthmatics. |
| Metoprolol | Adrenergic Antagonist
beta-Antagonist, beta1-Selective |
Local anesthetic membrane-stabilizing activity. Cardioselective: safer for use with asthmatics. |
| Butoxamine | Adrenergic Antagonist
beta-Antagonist, beta2-Selective |
The only beta2-selective drug. No current therapeutic use. |
| Carteolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Has partial beta-agonist activity. |
| Levobunolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Decrease aqueous humour production, used to treat open-angle glaucoma. |
| Nadolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Has particularly long half-life and duration of action. |
| Penbutolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Has partial beta-agonist activity. |
| Pindolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Has good oral bioavailability. Has partial beta-agonist activity. Local anesthetic membrane-stabilizing activity. |
| Propanolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Undergoes extensive first-pass metabolism. Lipophilic, readily crosses BBB,
used to treat migraines and other CNS disorders.
Local anesthetic membrane-stabilizing activity. |
| Timolol | Adrenergic Antagonist
beta-Antagonist, non-selective |
Decrease aqueous humour production, used to treat open-angle glaucoma. Local anesthetic membrane-stabilizing activity. |
| Bretylium | Adrenergic Antagonist, Indirect
NE-depleting agent |
Similar to Guanethidine. Also has direct anti-arrhythmic effects on heart. |
| Guanadrel | Adrenergic Antagonist, Indirect
NE-depleting agent |
Similar to Guanethidine but has a shorter duration of action. |
| Guanethidine | Adrenergic Antagonist, Indirect
NE-depleting agent |
Inhibits NE release and gradually depletes NE storage granules. Uptake I is required, so its effects are blocked by Cocaine. After 1-2 weeks of treatment, reduction of b.p., and often CO stays near normal. |
| Reserpine | Adrenergic Antagonist, Indirect
NE-depleting agent |
Blocks the transport of NE and Dopamine into vesicles, thus depleting their
stores. Effect is irreversible: a single dose depletes all amines until more can
be synthesized.
Side effects: Sedation, Parkinsonian symptoms, increased gastrin secretion, psychic depression. |
| Muscarine | Cholinergic Agonist, Direct
Muscarinic Alkaloid |
Prototype muscarinic agonist. Poison found in mushrooms, causing cholinergic hyper-activation. |
| Pilocarpine | Cholinergic Agonist, Direct
Muscarinic Alkaloid |
|
| Acetylcholine | Cholinergic Agonist, Direct
Muscarinic Choline ester |
LOW DOSE: Stimulate NO, vasodilation, reflex tachycardia
HIGH DOSE: Vasodilation, direct bradycardia. Extremely short-half life in-vitro due to abundant cholinesterase. |
| Arecholine | Cholinergic Agonist, Direct
Muscarinic Choline ester |
|
| Bethanechol | Cholinergic Agonist, Direct
Muscarinic Choline ester |
Resistant to cholinesterase, thus it has a longer half-life than ACh.
Does not cross blood-brain barrier; used in GI and GU tracts. |
| Carbachol | Cholinergic Agonist, Direct
Muscarinic Choline ester |
Resistant to cholinesterase, thus it has a longer half-life than ACh. Causes
release of endogenous ACh as well as being an agonist. It does cross BBB.
Direct application in eye: used to treat non-congestive wide-angle glaucoma. |
| Methacholine | Cholinergic Agonist, Direct
Muscarinic Choline ester |
Resistant to Acetylcholinesterase, but susceptible to other cholinesterases,
thus it has an intermediate half-life.
Primarily used as a diagnostic agent.. If muscarine is present, then SQ Methacholine will not produce expected cholinergic effects. |
| Succinylcholine | Cholinergic Agonist, Direct
Muscarinic Choline ester |
Binds to nicotinic receptors with higher affinity than ACh. Early on: muscle fasciculations. Later: paralysis due to depolarization blockade. |
| Nicotine | Cholinergic Agonist, Direct
Nicotinic |
Increases all autonomic outflow (nicotinic ganglionic stimulation). Also
stimulates adrenal medulla to release NE and Epi, further increasing
sympathetics.
Found in insecticides as well as cigarette smoke. At high (toxic) doses, it can cause depolarizing blockade of smooth and skeletal muscle. |
| Ambenonium | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Carbamate (Reversible) |
Quaternary ammonium compound, does not enter CNS. Still has some
adverse CNS effects.
Can be used to treat Myasthenia Gravis. |
| Demecarium | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Carbamate (Reversible) |
Quaternary ammonium compound, does not enter CNS.
Can be used in treatment of glaucoma. Longer duration of action. |
| Edrophonium | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Carbamate (Reversible) |
Very short-acting, used in diagnosis of Myasthenia Gravis. Edrophonium should decrease muscle strength. If it instead increases muscle strength, then MG is likely. If it makes matters worse, then suspect a cholinergic crisis (depolarizing blockade) |
| Neostigmine | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Carbamate (Reversible) |
Has a quaternary nitrogen and does enter CNS.
Can be used to treat Myasthenia Gravis. |
| Physostigmine | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Carbamate (Reversible) |
Is a tertiary nitrogen and does enter CNS. It is therefore used in treatment of Atropine poisoning. |
| Pyridostigmine | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Carbamate (Reversible) |
Quaternary ammonium compound, does not enter CNS.
Can be used to treat Myasthenia Gravis. |
| Echothiophate | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
Can be used in glaucoma treatment. |
| Isoflurophate (DFP) | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
Can be used in glaucoma treatment. |
| Malathion | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
Common insecticide. |
| Parathion | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
Common insecticide. |
| Sarin | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
Nerve gas. |
| Soman | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
Nerve gas. |
| Tabun | Cholinergic Agonist, Indirect
Cholinesterase Inhibitor Organophosphate (Irreversible) |
|
| Trimethaphan | Cholinergic Antagonist, Direct
Ganglionic Blocker Blocks NG receptors |
Blocks all autonomic responses. |
| Hexamethonium | Cholinergic Antagonist, Direct
Ganglionic Blocker Blocks NG receptors |
Prototypical ganglionic blocker. Blocks all autonomic reflex responses (generally, a reflex tachycardia or bradycardia) |
| Atropine | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Antidote to organophosphate poisoning, if it has already been more than a
half-hour.
Crosses BBB |
| Benztropine | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Crosses BBB |
| Cyclopentolate | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Crosses BBB |
| Homatropine | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Crosses BBB |
| Pirenzepine | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Crosses BBB |
| Scopolamine | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Can be given as a patch to treat motion sickness.
Crosses BBB |
| Trihexyphenidyl | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Crosses BBB |
| Tropicamide | Cholinergic Antagonist, Direct
Muscarinic Antagonist 3 Amine |
Crosses BBB |
| Atropine Methyl-nitrate | Cholinergic Antagonist, Direct
Muscarinic Antagonist 4 Amine |
Does not cross BBB |
| Glycopyrrolate | Cholinergic Antagonist, Direct
Muscarinic Antagonist 4 Amine |
Does not cross BBB |
| Ipratropium | Cholinergic Antagonist, Direct
Muscarinic Antagonist 4 Amine |
Does not cross BBB |
| Methscopolamine | Cholinergic Antagonist, Direct
Muscarinic Antagonist 4 Amine |
Does not cross BBB |
| Propantheline | Cholinergic Antagonist, Direct
Muscarinic Antagonist 4 Amine |
Does not cross BBB |
| Mecamylamine | Cholinergic Antagonist, Direct
Nicotinic Blocker |
|
| Curare (d-Tubocurarine) | Cholinergic Antagonist, Direct
Nicotinic Blocker Blocks Neuromuscular Junction |
Prototypical NMJ Antagonist. Causes flaccid paralysis of skeletal muscle.. It only blocks the NMJ -- not other nicotinic receptors, and not muscarinic! |
| Botulinum Toxin | Cholinergic Antagonist, Indirect | Prevents the release of ACh |
| Hemicholinium | Cholinergic Antagonist, Indirect | Prevents the sequestration of ACh into vesicles |
| Pralidoxime
(2-PAM) |
Cholinesterase Activator | Antidote to organophosphate poisoning, as long as it is administered within first half-hour, before aging occurs. |
| Mifepristone | Contraceptive
Anti-Progestin |
RU-486 morning-after pill. It is a weak partial agonist of progestin receptors. It induces abortion in first trimester (or morning after) by causing luteolysis, embryo detachment, and inducing menstruation. |
| Demulen | Contraceptive
Combined Oral Contraceptive |
Ethinyl estradiol + ethynodiol diacetate |
| Lo/ovral | Contraceptive
Combined Oral Contraceptive |
Ethinyl estradiol + dl-Norgestrel |
| Loestrin | Contraceptive
Combined Oral Contraceptive |
Ethinyl estradiol + norethindrone |
| Ortho-Novum | Contraceptive
Combined Oral Contraceptive |
Ethinyl Estradiol + Norethindrone |
| Ovulen | Contraceptive
Combined Oral Contraceptive |
Mestranol + ethynodiol diacetate |
| Diethylstilbestrol | Contraceptive
Estrogen |
Non-steroidal, but it has estrogen activity. No longer used in contraceptives because it can cause reproductive cancers in daughters born to mothers taking the pill. Today it is only used as a post-coital ("morning after") contraceptive. |
| Ethinyl Estradiol | Contraceptive
Estrogen |
Estradiol + Ethinyl at 17-position. Mainstay of oral contraceptives. |
| Mestranol | Contraceptive
Estrogen |
Metabolic precursor to Ethinyl Estradiol. |
| Ethynodiol Diacetate | Contraceptive
Progestin |
Used in combined oral contraceptives. Can have androgenic side-effects (acne, hirsutism) |
| l-Norgestrel | Contraceptive
Progestin |
Norplant implanted contraceptive. Used in combined oral contraceptives. Can have androgenic side-effects (acne, hirsutism). Has the most potent progestine properties. |
| Medroxyprogesterone | Contraceptive
Progestin |
When given IM, it is the Depo Provera contraceptive shot. Very resistant to
metabolism when given IM (long lasting). It is close in structure to Progesterone and has no androgenic side-effects.
It is the only progestin used in combined post-menopausal hormone replacement therapy. |
| Norethindrone | Contraceptive
Progestin |
Used in combined oral contraceptives. Can have androgenic side-effects (acne, hirsutism) |
| Norethynodrel | Contraceptive
Progestin |
Used in combined oral contraceptives. Can have androgenic side-effects (acne, hirsutism). Has no androgenic effects. Most extensive estrogenic activity, with the least progestin activity. |
| Metformin | Diabetes
Biguanide |
Mechanism of action unknown. Their hypoglycemic activity does not depend on the presence of functional beta-cells. |
| Isophane (NPH) Insulin | Diabetes
Insulin Intermediate-acting |
Cloudy solution. Protease reacts with the protamine to release the insulin. Later onset and longer duration. |
| Lente Insulin | Diabetes
Insulin Intermediate-acting |
Cloudy solution. Insulin precipitated with Zinc in acetate buffer. |
| Ultralente Insulin | Diabetes
Insulin Long-acting |
Cloudy solution. Poorly soluble complex of zinc and insulin. Due to poor manageability, used only with Type I Diabetics. |
| Bovine Insulin | Diabetes
Insulin Short-acting |
Regular insulin, clear solution. Rapid onset and duration of a few hours. It is taken before meals for its immediate effects. |
| Humulin | Diabetes
Insulin Short-acting |
Regular insulin, clear solution. Rapid onset and duration of a few hours. It is taken before meals for its immediate effects. |
| Porcine Insulin | Diabetes
Insulin Short-acting |
Regular insulin, clear solution. Rapid onset and duration of a few hours. It is taken before meals for its immediate effects. |
| Acetohexamide | Diabetes
Sulfonylurea |
Relatively long-acting. |
| Chlorpropamide | Diabetes
Sulfonylurea |
Very long-acting. |
| Glipizide | Diabetes
Sulfonylurea |
"Second-generation" sulfonylurea. |
| Glyburide | Diabetes
Sulfonylurea |
"Second-generation" sulfonylurea. More potent ad fewer side-effects. Short
half-life, yet it has a long action of about 24 hrs.
Contraindicated in hepatic or renal impairment. |
| Tolazamide | Diabetes
Sulfonylurea |
Relatively long-acting. |
| Tolbutamide | Diabetes
Sulfonylurea |
Relatively long-acting. |
| Carbidopa | Dopamine Antagonist, Indirect
Dopamine-Decarboxylase Inhibitor |
Prevents the formation of Dopamine. |
| Paramethasone | Glucocorticoid
Intermediate-acting |
No salt-retaining activity. |
| Triamcinolone | Glucocorticoid
Intermediate-acting |
No salt-retaining activity. |
| Betamethasone | Glucocorticoid
Long-acting |
Very potent. No salt-retaining activity. |
| Dexamethasone | Glucocorticoid
Long-acting |
Very potent. No salt-retaining activity. |
| Cortisone | Glucocorticoid
Short-acting |
Some salt-retaining activity (i.e. Aldosterone cross-reactivity) |
| Hydrocortisone (same as endogenous Cortisol) | Glucocorticoid
Short-acting |
|
| Meprednisone | Glucocorticoid
Short-acting |
Some salt-retaining activity (i.e. Aldosterone cross-reactivity) |
| Methylprednisolone | Glucocorticoid
Short-acting |
Some salt-retaining activity (aldosterone cross-reactivity) |
| Prednisolone | Glucocorticoid
Short-acting |
Some salt-retaining activity (aldosterone cross-reactivity) |
| Prednisone | Glucocorticoid
Short-acting |
Some salt-retaining activity (aldosterone cross-reactivity) |
| Cosyntropin (Adrenal-Corticotropin Hormone (ACTH)) | Hormone
ACTH |
Used Diagnostically to evaluate adrenal insufficiency. If Cortisol does not respond to exogenous ACTH, then the problem is primary. |
| Metyrapone | Hormone
Anti-Cortisol |
Inhibits 11beta-Dehydroxylase, the final step in the formation of Cortisol,
thus preventing formation of Cortisol.
Used diagnostically to confirm secondary adrenal insufficiency. Give Metyrapone, and look for increase in ACTH levels. No increase in ACTH indicates secondary adrenal insufficiency. |
| Clomiphene | Hormone
Anti-Estrogen |
It is used to stimulate ovulation, but the mechanism is not completely understood. Proposed mech: blocks estrogen effects on hypothalamus ------> promote GnRH ------> promotes ovulation. |
| Tamoxifen | Hormone
Anti-Estrogen |
Used to treat breast cancer. Antagonizes the action of estrogen on breast tissue. |
| Iodide, I- | Hormone
Anti-Thyroid |
Exogenous I- temporarily (short-term) inhibits the proteolysis of thyroglobulin, preventing release of T4. Used to treat acute thyroid storm.
Also used before surgery, to make the Thyroid smaller and more firm. |
| Radio-Iodine, 131I | Hormone
Anti-Thyroid |
Used to treat hyperthyroidism. The 131I gets concentrated in the Thyroid,
where it diffusely kills thyroid cells.
Ultimately it will lead to hypothyroidism, which can then be treated with T4. |
| Perchlorate (ClO4-) | Hormone
Anti-Thyroid Ionic Inhibitor |
Inhibits uptake of iodide into the Thyroid.
In large doses, this drug causes aplastic anemia. Only use in small doses. |
| Thiocyanate (SCN-) | Hormone
Anti-Thyroid Ionic Inhibitor |
Inhibits uptake of iodide into the Thyroid. |
| Carbimazole | Hormone
Anti-Thyroid Thionamide |
Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed. |
| Methimazole | Hormone
Anti-Thyroid Thionamide |
Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic
effect is delayed.
This is the metabolic by-product of Carbimazole. |
| Propylthiouracil | Hormone
Anti-Thyroid Thionamide |
Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic
effect is delayed.
Also inhibits peripheral conversion of T4 to T3. |
| Calcimar | Hormone
Calcium-regulation |
Calcitonin obtained from salmon. |
| Calcitriol (Vitamin-D) | Hormone
Calcium-regulation |
Used to treat Rickets, Hypoparathyroidism, Osteomalacia. |
| Cibacalcin (Calcitonin) | Hormone
Calcium-regulation |
Used to help treat hyperparathyroidism, hypercalcemia, and Paget's Disease (characterized by increased skeletal remodeling). |
| Dihydrotachysterol | Hormone
Calcium-regulation |
Vitamin-D analogue. More effective than Vit-D because it bypasses renal mechanisms of metabolic control. |
| Parathyroid Hormone (PTH) | Hormone
Calcium-regulation |
Used diagnostically to diagnose pseudo hypothyroidism, a disorder characterized by insensitivity to PTH. |
| Corticotropin Releasing Hormone (CRH) | Hormone
CRH |
|
| Estradiol, Estrone | Hormone
Estrogen |
Mixture of equine natural estrogens are used in post-menopausal hormone
replacement therapy.
The equine estrogen has one extra double-bond and is hence called a "conjugated estrogen." |
| Urofollitropin | Hormone
FSH |
Natural FSH extracted from urine. Used to treat infertility. |
| Somatrem (Growth Hormone, GH, Somatomedin) | Hormone
GH |
Given as replacement therapy, only to children with open epiphyses. Contraindicated in people with closed epiphyses.
Biosynthetic, identical to endogenous GH |
| Sermatorelin (Growth-Hormone Releasing Hormone, GHRH) | Hormone
GHRH |
Given diagnostically, to diagnose primary (pituitary) or secondary (hypothalamic) GH deficiency (Dwarfism) |
| Gonadorelin (Gonadotropin-Releasing Hormone, GnRH) | Hormone
GnRH |
Very short half-life of 4 minutes. Can be given intranasally, IV, or SQ.
Pulsatile administrated every 3 or 4 hrs.
Used to treat hypogonadism in men or women, delayed puberty, and cryptorchidism. |
| Leuprolide | Hormone
GnRH Analogue |
Longer half-life of about 3 hrs. Can be given in pulsatile fashion, or continuously.
Continuous administration: used to slow down precocious puberty, or used to supress endogenous GnRH release in in-vitro fertilization. |
| Nafarelin | Hormone
GnRH Analogue |
Longer half-life of about 3-hrs. |
| Human Menopausal Gonadotropins (hMG) | Hormone
Menotropin |
Partially degraded mixture of both FSH + LH. They still retain some FSH +
LH activity. Administered IM to promote follicular growth, treat infertility.
Can be used to treat infertility in both men and women. |
| Human Chorionic Gonadotropin (hCG) | Hormone
Menotropin |
Obtained from urine of pregnant women. Closely related to LH. Given IM at mid-cycle (or whenever follicle is adequate developed) to mimic the luteal surge, to try to induce ovulation and treat infertility. |
| Oxytocin | Hormone
Oxytocin |
Given IV to induce labor in mild eclampsia or incomplete abortion. Given IM to control post-partum bleeding. Given intranasally as needed to induce lactation. |
| Prolactin | Hormone
Prolactin |
No therapeutic use. |
| Bromocriptine | Hormone
Prolactin Antagonist Dopamine Agonist |
Dopamine agonist ------> suppress Prolactin. Used to treat hyperprolactinemia. |
| Thyroxine (T4) | Hormone
Thyroxine |
Given orally to treat hypothyroidism. T4 is given -- not T3, which is too potent and has cardiotoxic side-effects. |
| Protirelin (Thyrotropin-Releasing Hormone, TRH) | Hormone
TRH |
Used diagnostically to distinguish between primary and secondary hypothyroidism. |
| Thyroid-Stimulating Hormone (TSH) | Hormone
TSH |
Used to promote uptake of radioactive 131I, to treat Thyroid carcinoma. Derived from bovine pituitaries. |
| Vasopressin (ADH) | Hormone
Vasopressin |
Used to treat Diabetes Insipidus. Administered IV, IM, intranasally.
V1 Receptors: Vascular vasoconstriction. V2 Receptors: Tubular reabsorption of water. |
| Desmopressin | Hormone
Vasopressin Analogue |
Synthetic Vasopressin analogue. Longer-acting then Vasopressin. |
| Desoxycorticosterone acetate | Mineralocorticoid | |
| Fludrocortisone | Mineralocorticoid | Used to replace Aldosterone activity in cases of adrenal insufficiency. |