| Drug Name |
Category |
Mechanism, Indications, Adverse
Effects, Unique Properties |
| Phenoxy benzamine |
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. |
| Hexame thonium |
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 |
| Methsco polamine |
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. |
| Medroxypro gesterone |
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. |
