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Pharmacology Test 1 Drug List

Alphabetical

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Drug Name Category Mechanism, Indications, Adverse Effects, Unique Properties
Acebutolol Adrenergic Antagonist

beta-Antagonist, beta1-Selective

Has partial beta-agonist activity. Local anesthetic membrane-stabilizing activity.

Cardioselective: safer for use with asthmatics.

Acetohexamide Diabetes

Sulfonylurea

Relatively long-acting.
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.

Albuterol Adrenergic Agonist, Direct

beta2-selective

Bronchodilator
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.

Amitriptyline Adrenergic Agonist, Indirect

NE-Potentiating Agent

Uptake-I Inhibitor, Tri-Cyclic Antidepressant

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.
Arecholine Cholinergic Agonist, Direct

Muscarinic

Choline ester

Atenolol Adrenergic Antagonist

beta-Antagonist, beta1-Selective

Cardioselective: safer for use with asthmatics.
Atropine Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Antidote to organophosphate poisoning, if it has already been more than a half-hour.

Crosses BBB

Atropine Methyl-nitrate Cholinergic Antagonist, Direct

Muscarinic Antagonist

4 Amine

Does not cross BBB
Benztropine Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Crosses BBB
Betamethasone Glucocorticoid

Long-acting

Very potent. No salt-retaining activity.
Betaxolol Adrenergic Antagonist

beta-Antagonist, beta1-Selective

Decrease aqueous humour production, used to treat open-angle glaucoma. Cardioselective: safer for use with asthmatics.
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.

Bitoterol Adrenergic Agonist, Direct

beta2-selective

Bronchodilator. Prodrug is hydrolyzed in the lung by esterases to its active form, colterol.
Botulinum Toxin Cholinergic Antagonist, Indirect Prevents the release of ACh
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.
Bretylium Adrenergic Antagonist, Indirect

NE-depleting agent

Similar to Guanethidine. Also has direct anti-arrhythmic effects on heart.
Bromocriptine Hormone

Prolactin Antagonist

Dopamine Agonist

Dopamine agonist ------> suppress Prolactin. Used to treat hyperprolactinemia.
Butoxamine Adrenergic Antagonist

beta-Antagonist, beta2-Selective

The only beta2-selective drug. No current therapeutic use.
Calcimar Hormone

Calcium-regulation

Calcitonin obtained from salmon.
Calcitriol (Vitamin-D) Hormone

Calcium-regulation

Used to treat Rickets, Hypoparathyroidism, Osteomalacia.
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.

Carbidopa Dopamine Antagonist, Indirect

Dopamine-Decarboxylase Inhibitor

Prevents the formation of Dopamine.
Carbimazole Hormone

Anti-Thyroid

Thionamide

Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed.
Carteolol Adrenergic Antagonist

beta-Antagonist, non-selective

Has partial beta-agonist activity.
Chlorpropamide Diabetes

Sulfonylurea

Very long-acting.
Cibacalcin (Calcitonin) Hormone

Calcium-regulation

Used to help treat hyperparathyroidism, hypercalcemia, and Paget's Disease (characterized by increased skeletal remodeling).
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.
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.

Clorgyline Adrenergic Agonist, Indirect

NE-Potentiating Agent

MAO Inhibitor

MAO-A-selective inhibitor.
Cocaine Adrenergic Agonist, Indirect

NE-Potentiating Agent

Uptake I Inhibitor

Blocks Uptake I (NE reuptake), thus potentiating the effects of NE.
Corticotropin Releasing Hormone (CRH) Hormone

CRH

Cortisone Glucocorticoid

Short-acting

Some salt-retaining activity (i.e. 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.
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!
Cyclopentolate Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Crosses BBB
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.

Demulen Contraceptive

Combined Oral Contraceptive

Ethinyl estradiol + ethynodiol diacetate
Deprenyl Adrenergic Agonist, Indirect

NE-Potentiating Agent

MAO Inhibitor

MAO-B-selective inhibitor.
Desmopressin Hormone

Vasopressin Analogue

Synthetic Vasopressin analogue. Longer-acting then Vasopressin.
Desoxycorticosterone acetate Mineralocorticoid
Dexamethasone Glucocorticoid

Long-acting

Very potent. No salt-retaining activity.
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.
Dihydrotachysterol Hormone

Calcium-regulation

Vitamin-D analogue. More effective than Vit-D because it bypasses renal mechanisms of metabolic control.
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).

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
Doxazosin Adrenergic Antagonist

alpha-Antagonist, alpha1-Selective

Similar to Prazosin but with longer half-life.
Echothiophate Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Can be used in glaucoma treatment.
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)
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.

Epinephrine Adrenergic Agonist, Direct

Non-selective (alpha1, alpha2, beta1, beta2)

Increase b.p. (alpha1) and direct tachycardia (beta1).
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.

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."

Ethinyl Estradiol Contraceptive

Estrogen

Estradiol + Ethinyl at 17-position. Mainstay of oral contraceptives.
Ethynodiol Diacetate Contraceptive

Progestin

Used in combined oral contraceptives. Can have androgenic side-effects (acne, hirsutism)
Fludrocortisone Mineralocorticoid Used to replace Aldosterone activity in cases of adrenal insufficiency.
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.

Glycopyrrolate Cholinergic Antagonist, Direct

Muscarinic Antagonist

4 Amine

Does not cross BBB
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.

Guanabenz Adrenergic Agonist, Direct

alpha2-selective

It is an indirect adrenergic antagonist, as it decreases sympathetic outflow.
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.
Guanfacine Adrenergic Agonist, Direct

alpha2-selective

It is an indirect adrenergic antagonist, as it decreases sympathetic outflow.
Hemicholinium Cholinergic Antagonist, Indirect Prevents the sequestration of ACh into vesicles
Hexamethonium Cholinergic Antagonist, Direct

Ganglionic Blocker

Blocks NG receptors

Prototypical ganglionic blocker. Blocks all autonomic reflex responses (generally, a reflex tachycardia or bradycardia)
Homatropine Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Crosses BBB
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.
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.

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.
Hydrocortisone (same as endogenous Cortisol) Glucocorticoid

Short-acting

Imipramine Adrenergic Agonist, Indirect

NE-Potentiating Agent

Uptake-I Inhibitor, Tri-Cyclic Antidepressant

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.

Ipratropium Cholinergic Antagonist, Direct

Muscarinic Antagonist

4 Amine

Does not cross BBB
Isoethanine Adrenergic Agonist, Direct

beta2-selective

Bronchodilator
Isoflurophate (DFP) Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Can be used in glaucoma treatment.
Isophane (NPH) Insulin Diabetes

Insulin

Intermediate-acting

Cloudy solution. Protease reacts with the protamine to release the insulin. Later onset and longer duration.
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.
l-Norgestrel Contraceptive

Progestin

Norplant implanted contraceptive. Used in combined oral contraceptives. Can have androgenic side-effects (acne, hirsutism). Has the most potent progestin properties.
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.

Lente Insulin Diabetes

Insulin

Intermediate-acting

Cloudy solution. Insulin precipitated with Zinc in acetate buffer.
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.

Levobunolol Adrenergic Antagonist

beta-Antagonist, non-selective

Decrease aqueous humour production, used to treat open-angle glaucoma.
Lo/ovral Contraceptive

Combined Oral Contraceptive

Ethinyl estradiol + dl-Norgestrel
Loestrin Contraceptive

Combined Oral Contraceptive

Ethinyl estradiol + norethindrone
Malathion Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Common insecticide.
Mecamylamine Cholinergic Antagonist, Direct

Nicotinic Blocker

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.

Meprednisone Glucocorticoid

Short-acting

Some salt-retaining activity (i.e. Aldosterone cross-reactivity)
Mestranol Contraceptive

Estrogen

Metabolic precursor to Ethinyl Estradiol.
Metaproterenol Adrenergic Agonist, Direct

beta2-selective

Bronchodilator
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.

Metformin Diabetes

Biguanide

Mechanism of action unknown. Their hypoglycemic activity does not depend on the presence of functional beta-cells.
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.

Methamphetamine Adrenergic Agonist, Indirect

NE-Releasing Agent

Amphetamine

Promotes release of NE from pre-synaptic neuron. More pronounced CNS effects than amphetamine.
Methimazole Hormone

Anti-Thyroid

Thionamide

Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed.

This is the metabolic by-product of Carbimazole.

Methoxamine Adrenergic Agonist, Direct

alpha1-selective

Used to maintain blood pressure during anesthesia. Produces fewer arrhythmias than other drugs.
Methscopolamine Cholinergic Antagonist, Direct

Muscarinic Antagonist

4 Amine

Does not cross BBB
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.
Methylphenidate Adrenergic Agonist, Indirect

NE-Releasing Agent

Amphetamine

Similar to Methamphetamine, with abuse potential.
Methylprednisolone Glucocorticoid

Short-acting

Some salt-retaining activity (aldosterone cross-reactivity)
Metoprolol Adrenergic Antagonist

beta-Antagonist, beta1-Selective

Local anesthetic membrane-stabilizing activity. Cardioselective: safer for use with asthmatics.
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.

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.
Muscarine Cholinergic Agonist, Direct

Muscarinic

Alkaloid

Prototype muscarinic agonist. Poison found in mushrooms, causing cholinergic hyper-activation.
Nadolol Adrenergic Antagonist

beta-Antagonist, non-selective

Has particularly long half-life and duration of action.
Nafarelin Hormone

GnRH Analogue

Longer half-life of about 3-hrs.
Naphazoline Adrenergic Agonist, Direct

alpha1-selective

Used to induce mydriasis before ophthalmic exam.
Neostigmine Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Carbamate (Reversible)

Has a quaternary nitrogen and does enter CNS.

Can be used to treat Myasthenia Gravis.

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.

Norepinephrine Adrenergic Agonist, Direct

alpha1, alpha2, beta1

Increase b.p. ------> reflex bradycardia.. If reflexes are blocked by Hexamethonium, then you see a direct tachycardia.
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.
Ortho-Novum Contraceptive

Combined Oral Contraceptive

Ethinyl Estradiol + Norethindrone
Ovulen Contraceptive

Combined Oral Contraceptive

Mestranol + ethynodiol diacetate
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.
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.
Paramethasone Glucocorticoid

Intermediate-acting

No salt-retaining activity.
Parathion Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Common insecticide.
Parathyroid Hormone (PTH) Hormone

Calcium-regulation

Used diagnostically to diagnose pseudo hypothyroidism, a disorder characterized by insensitivity to PTH.
Pargyline Adrenergic Agonist, Indirect

NE-Potentiating Agent

MAO Inhibitor

Non-selective MAO inhibitor.
Pemoline Adrenergic Agonist, Indirect

NE-Releasing Agent

Amphetamine

Similar to Methamphetamine, with abuse potential.
Penbutolol Adrenergic Antagonist

beta-Antagonist, non-selective

Has partial beta-agonist activity.
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.

Phenmetrazine Adrenergic Agonist, Indirect

NE-Releasing Agent

Amphetamine

Similar to Methamphetamine, with abuse potential.
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.

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.

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.
Pilocarpine Cholinergic Agonist, Direct

Muscarinic

Alkaloid

Pindolol Adrenergic Antagonist

beta-Antagonist, non-selective

Has good oral bioavailability. Has partial beta-agonist activity. Local anesthetic membrane-stabilizing activity.
Pirbuterol Adrenergic Agonist, Direct

beta2-selective

Bronchodilator
Pirenzepine Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Crosses BBB
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.
Pralidoxime

(2-PAM)

Cholinesterase Activator Antidote to organophosphate poisoning, as long as it is administered within first half-hour, before aging occurs.
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.
Prednisolone Glucocorticoid

Short-acting

Some salt-retaining activity (aldosterone cross-reactivity)
Prednisone Glucocorticoid

Short-acting

Some salt-retaining activity (aldosterone cross-reactivity)
Prolactin Hormone

Prolactin

No therapeutic use.
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.

Propantheline Cholinergic Antagonist, Direct

Muscarinic Antagonist

4 Amine

Does not cross BBB
Propylthiouracil Hormone

Anti-Thyroid

Thionamide

Inhibits organification (iodination) steps of Thyroid synthesis. Therapeutic effect is delayed.

Also inhibits peripheral conversion of T4 to T3.

Protirelin (Thyrotropin-Releasing Hormone, TRH) Hormone

TRH

Used diagnostically to distinguish between primary and secondary hypothyroidism.
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.

Pyridostigmine Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Carbamate (Reversible)

Quaternary ammonium compound, does not enter CNS.

Can be used to treat Myasthenia Gravis.

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.

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.

Ritodrine Adrenergic Agonist, Direct

beta2-selective

Used to relax the uterus during labor.
Sarin Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Nerve gas.
Scopolamine Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Can be given as a patch to treat motion sickness.

Crosses BBB

Sermatorelin (Growth-Hormone Releasing Hormone, GHRH) Hormone

GHRH

Given diagnostically, to diagnose primary (pituitary) or secondary (hypothalamic) GH deficiency (Dwarfism)
Soman Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Nerve gas.
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

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.
Tabun Cholinergic Agonist, Indirect

Cholinesterase Inhibitor

Organophosphate (Irreversible)

Tamoxifen Hormone

Anti-Estrogen

Used to treat breast cancer. Antagonizes the action of estrogen on breast tissue.
Terazosin Adrenergic Antagonist

alpha-Antagonist, alpha1-Selective

Similar to Prazosin but with longer half-life.
Terbutaline Adrenergic Agonist, Direct

beta2-selective

Bronchodilator
Thiocyanate (SCN-) Hormone

Anti-Thyroid

Ionic Inhibitor

Inhibits uptake of iodide into the Thyroid.
Thyroid-Stimulating Hormone (TSH) Hormone

TSH

Used to promote uptake of radioactive 131I, to treat Thyroid carcinoma. Derived from bovine pituitaries.
Thyroxine (T4) Hormone

Thyroxine

Given orally to treat hypothyroidism. T4 is given -- not T3, which is too potent and has cardiotoxic side-effects.
Timolol Adrenergic Antagonist

beta-Antagonist, non-selective

Decrease aqueous humour production, used to treat open-angle glaucoma. Local anesthetic membrane-stabilizing activity.
Tolazamide Diabetes

Sulfonylurea

Relatively long-acting.
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.

Tolbutamide Diabetes

Sulfonylurea

Relatively long-acting.
Tranylcypromine Adrenergic Agonist, Indirect

NE-Potentiating Agent

MAO Inhibitor

Non-selective MAO inhibitor.
Triamcinolone Glucocorticoid

Intermediate-acting

No salt-retaining activity.
Trihexyphenidyl Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Crosses BBB
Trimethaphan Cholinergic Antagonist, Direct

Ganglionic Blocker

Blocks NG receptors

Blocks all autonomic responses.
Tropicamide Cholinergic Antagonist, Direct

Muscarinic Antagonist

3 Amine

Crosses BBB
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.

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.
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.
Urofollitropin Hormone

FSH

Natural FSH extracted from urine. Used to treat infertility.
Vasopressin (ADH) Hormone

Vasopressin

Used to treat Diabetes Insipidus. Administered IV, IM, intranasally.

V1 Receptors: Vascular vasoconstriction. V2 Receptors: Tubular reabsorption of water.

Xylometolazine Adrenergic Agonist, Direct

alpha1, alpha2

Topical nasal decongestant.
Yohimbine Adrenergic Antagonist

alpha-Antagonist, alpha2-selective

The only alpha2-selective antagonist there is. May be useful in autonomic insufficiency.

b

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