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FHD Pharm
Cholinergic & Adrenergic, Agonist & Antagonists
| Drug | Class | Mechanism |
|---|---|---|
| Sildenafil | -afil Phosphodiesterase (PDE) inhibitor | Inhibits the conversion of cyclic GMP to 5'-GMP. This decreases intracellular Ca++ and causes the uncoupling of actin and myosin causing vasodilation |
| Tadalafil | -afil Phosphodiesterase (PDE) inhibitor | Inhibits the conversion of cyclic GMP to 5'-GMP. This decreases intracellular Ca++ and causes the uncoupling of actin and myosin causing vasodilation |
| Avanafil | -afil Phosphodiesterase (PDE) inhibitor | Inhibits the conversion of cyclic GMP to 5'-GMP. This decreases intracellular Ca++ and causes the uncoupling of actin and myosin causing vasodilation |
| Acetylcholine | no root Muscarinic agonist | Direct neurotransmitter for nicotinic and muscarinic receptors. |
| Muscarine | no root Muscarinic agonist | Mimics acetylcholine. No effect on nicotinic receptors. |
| Pilocarpine | no root Muscarinic agonist | Mimics acetylcholine. No effect on nicotinic receptors. |
| Bethanechol | no root Muscarinic agonist | Mimics acetylcholine. No effect on nicotinic receptors. |
| Methancholine | no root Muscarinic agonist | Mimics acetylcholine has an effect on both nicotinic and muscarinic receptors. |
| Botulinum Toxin | Blocks exocytosis of presynaptic vesicles thus blocking acetylcholine release | |
| Atropine | no root Muscarinic antagonist & AChE Poisoning Antidote | Competes for the same binding site as ACh via competitive inhibition. Cannot cross the BBB. |
| Scopolamine | no root Muscarinic antagonist | Competes for the same binding site as ACh via competitive inhibition. Can cross the BBB. Treats motion sickness. |
| Ipratropium | no root Muscarinic antagonist | Competes for the same binding site as ACh via competitive inhibition. Cannot cross the BBB. |
| Tolterodine | no root Muscarinic antagonist | Competes for the same binding site as ACh via competitive inhibition. Used to treat overactive bladder, has no selectivity for bladder muscarinic receptors. |
| Endrophonium | no root Acetylcholine-Esterase Inhibitor | Very short duration of action |
| Neostigmine | -stigmine Acetylcholine-Esterase Inhibitor | Short duration of action. Difficulty passing through membranes. Poorly absorbed from GI tract/skin and does not cross the BBB. Primarily at the NM junction. |
| Physostigmine | -stigmine Acetylcholine-Esterase Inhibitor | Short duration of action. Difficulty passing through membranes. Well absorbed from the gut and crosses the BBB. Primarily at the NM junction. |
| Pyridostigmine | -stigmine Acetylcholine-Esterase Inhibitor | Helps to saturate AChE enzyme so that chemical warfare agents will have limited ability to occupy the enzyme. |
| Echothiophate | no root Acetylcholine-Esterase Inhibitor | Acts on M3 muscarinic receptor. Produces miosis in the eyes. |
| Sarin | no root Acetylcholine-Esterase Inhibitor | Organophosphate, irreversibe AChE inhibitor |
| Malathion | no root Acetylcholine-Esterase Inhibitor | Organophosphate, irreversibe AChE inhibitor |
| Pralidoxime (2-PAM) | no root AChE Poisoning Antidote | AChE re-activator. Used to treat poisoning from organophosphates |
| Nicotine | no root Nicotinic Agonist | Binds to active sites on nicotinic channel, (mimicking acetylcholine). Stimulates reticular activating system and dopamine release. |
| Varenicline | no root Partial Nicotinic Agonist | Acts as a partial agonist at Ach receptors in the CNS. Blocks binding of nicotine and blocks positive reinforcement of nicotine through smoking. |
| Hexamethonium | no root Non-Depolarizing Ganglionic Agonist | |
| Succinylcholine | no root Depolarizing Nicotinic NMJ antagonist | Binds to nicotinic receptors in the neuromuscular junction leaves it open. |
| Tubocurarine | no root Non-Depolarizing Nicotinic NMJ antagonist | Competetive nicotinic receptor antagonist at the neuromuscular junction. Produces partial paralysis. Effects start at periphery and moves in. Diaphragm is last to paralyze. |
| Methyldopa | no root Indirect Adrenergic agonist | Enters the enzymatic path that produces NE from Dopamine. Forms a false transmitter that displaces NE and is released upon adrenergic stimulation. One of few drugs for pregnancy hypertension. |
| Cocaine | no root Indirect Adrenergic agonist | Blocks the NET reuptake transporter. More transmitter than normal remains in the synapse resulting in over stimulation. |
| Phenylephrine | no root Alpha agonist | Selective to the alpha 1 receptor. Activates beta receptors only at very high concentrations. |
| Tyramine | no root Indirect Adrenergic agonist | Displaces norepinephrine from sympathetic nerve endings, Overwhelms NET causing it to run in reverse and dump NE into the synaptic cleft. |
| Ephedrine | no root Indirect Adrenergic agonist | Displaces norepinephrine from sympathetic nerve endings, Overwhelms NET causing it to run in reverse and dump NE into the synaptic cleft. |
| Amphetamine | no root Indirect Adrenergic agonist | Displaces norepinephrine from sympathetic nerve endings, Overwhelms NET causing it to run in reverse and dump NE into the synaptic cleft. |
| Clonidine | no root Alpha agonist | Selective to the alpha 2 receptor. Stimulates alpha adrenergic receptors in the CV control centers of the CNS to reduce sympathetic nerve outflow and blood pressure. |
| Isoproterenol | no root Beta agonist | Nonselective beta receptor agonist with low affinity for alpha receptors. Relaxes all smooth muscle. |
| Dobutamine | no root Beta agonist | Selective to the beta 1 receptor. Positive inotropic effect on the heart. Increased CO and little change in total peripheral vascular resistance |
| Terbutiline | no root Beta agonist | Selective to beta 2 receptor. |
| Albuterol | no root Beta agonist | Selective to beta 2 receptor. |
| Mirabegron | no root Beta agonist | Selective to beta 3 receptor. It relaxes smooth muscle in the urinary bladder. |
| Phentolamine | no root Alpha blocker | Nonselective alpha blocker. Competitive inhibition. |
| Phenoxybenzamine | no root Alpha blocker | Selects alpha 1 over alpha 2. Irreversible antagonist. |
| Prazosin | no root Alpha blocker | Selective for alpha 1 receptors. Competitive inhibition. |
| Tamsulosin | no root Alpha blocker | Selective for alpha 1 receptive. Competitive inhibition. |
| Propanolol | -olol Beta blocker | Nonspecific beta-blocker antagonist |
| Metoprolol | -olol Beta blocker | Selective for beta 1. |
| Carvedilol | no root Mixed alpha/beta blocker | Selective for alpha and beta blockade, activation of NO, anti-oxidant properties, and vasodilator properties |
| Metyrosine | no root Indirect Adrenergic agonist | Modulates the synthesis of NE. Does not dump all NE into nerve synapse. |
| Reserpine | no root Indirect Adrenergic antagonist | Inhibits VMAT transporter and depletes the NE concentration in nerve endings. It dumps massive amounts NE into nerve synapse to deplete concentration. |
| Bretylium | no root Indirect Adrenergic antagonist | Modulates NE release. Depletes the NE concentration in nerve endings by dumping massive amounts NE into nerve synapse to deplete concentration. |
| Guanethidine | no root Indirect Adrenergic antagonist | Modulates NE release. Depletes the NE concentration in nerve endings by dumping massive amounts NE into nerve synapse to deplete concentration. |
| Methotrexate | no root Folate Antagonist | Keeps folate from doing its job and thus slows down cancer cell from growing |
| 5-Fluorouracil | no root Pyrimidine pathway inhibitor | Keeps DNA from Replicating |
| 6-Mercaptopurine | no root Purine Pathway inhibitor | Keeps DNA from Replicating |
| Cyclophosphamide | no root Alkylating agent | Nitrousurea compound which can alkalize proteins in the cell |
| Cisplatin | no root Alkylating agent | Platinum compound which can alkalize proteins in the cell |
| Daunorubicin | -rubicin Anthracycline | Intercalate into DNA, impair topoisomerase |
| Doxorubicin | -rubicin Anthracycline | Intercalate into DNA, impair topoisomerase |
| Bleomycin | no root Intercalating complex | Intercalate into DNA, promotes breakage |
| Topotecan | -tecan Camptothecin | Topoisomerase I inhibitor |
| Irinotecan | -tecan Camptothecin | Topoisomerase I inhibitor |
| Etoposide | no root Podophyllotoxins | Topoisomerase II inhibitor |
| Paclitaxel | -taxel Taxane | Mitotic Inhibitor by promoting microtubule assembly |
| Docetaxel | -taxel Taxane | Mitotic Inhibitor by promoting microtubule assembly |
| Vincristine | -stine Vinca alkaloids | Mitotic Inhibitor by disrupting microtubule assembly |
| Vinblastine | -stine Vinca alkaloids | Mitotic Inhibitor by disrupting microtubule assembly |
| Tamoxifen | -oxifen Hormone-Selective Estrogen Receptor Modulator | |
| Raloxifene | -oxifen Hormone-Selective Estrogen Receptor Modulator | |
| Rituximab | -mab Monoclonal Antibody | |
| Cetuximab | -mab Monoclonal Antibody | |
| Imatinib | -nib Protein kinase inhibitor | |
| Erlotinib | -nip Protein kinase inhibitor | |
| Vardenafil | -afil Phosphodiesterase (PDE) inhibitor | Inhibits the conversion of cyclic GMP to 5'-GMP. This decreases intracellular Ca++ and causes the uncoupling of actin and myosin causing vasodilation |
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