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FHD Pharm

Cholinergic & Adrenergic, Agonist & Antagonists

DrugClassMechanism
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
Created by: carchase