Term
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Definition
ACh/Muscarinic Agonist
limited use as a drug for the treatment of glaucoma
When it is administered systemically, it is very rapidly hydrolyzed by "pseudocholinesterase" in the plasma. |
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Term
| carbachol(Isopto Carbachol) |
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Definition
ACh/Muscarinic Agonist
resistant to hydrolysis by cholinesterases
stimulate both muscarinic and nicotinic receptors
topically in ophthalmology for the treatment of glaucoma |
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Term
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Definition
ACh/Muscarinic Agonist
stimulates muscarinic receptors with little effect at nicotinic receptors
pulmonary function testing in asthma |
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Term
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Definition
ACh/Muscarinic Agonist
resistant to rapid hydrolysis
direct muscarinic agonist with little effect at nicotinic receptors
stimulate GI motility and treat urinary retention |
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Term
| pilocarpine (Salagen, Ocusert Pilo) |
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Definition
ACh/Muscarinic Agonist
muscarinic agonist used in the treatment of glaucoma and xerostomia due to poor salivary secretion |
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Term
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Definition
Reversible Cholinesterase Inhibitors
quaternary ammonium compounds that doesn't enter the CNS
short acting (< 10 minutes) and is used in diagnosing myasthenia gravis (Tensilon test) |
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Term
| physostigmine (Eserine, Antilirium) |
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Definition
Reversible Cholinesterase Inhibitors
nonquaternary, so it can get into the CNS
used in treating poisoning with atropine or other antimuscarinic agents |
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Term
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Definition
Reversible Cholinesterase Inhibitors
quaternary ammonium compounds that doesn't enter the CNS
longer acting and are used in the treatment of myasthenia gravis |
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Term
| pyridostigmine (Mestinon) |
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Definition
Reversible Cholinesterase Inhibitors
quaternary ammonium compounds that doesn't enter the CNS
longer acting and are used in the treatment of myasthenia gravis
used by the military to protect troops against nerve agents used in chemical warfare |
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Term
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Definition
| Reversible Cholinesterase Inhibitors |
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Term
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Definition
| Reversible Cholinesterase Inhibitors |
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Term
| carbamate insecticides (e.g. *Carbaryl) |
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Definition
Reversible Cholinesterase Inhibitors
widely used insecticide
Not absorbed through the skin as much as parathion and malathion
Signs and symptoms of poisoning are similar to those of other cholinesterase inhibitors.
Treat poisoning with atropineand other symptomatic support. Pralidoxime is not useful in treating poisoning with carbaryl or other carbamate insecticides! |
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Term
| organophosphate insecticides (*parathion, malathion, diazinon and others) |
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Definition
Irreversible Cholinesterase Inhibitors
must be oxidized to active metabolites (paroxone and malaoxone). The conversion occurs more rapidly in insects than humans
can be absorbed through the skin
Signs and symptoms of poisoning are typical
Treat poisoning with *atropine, *pralidoxime, and other symptomatic support |
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Term
| DFP/diisopropylfurophosphate/Isoflurophate and echothiophate |
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Definition
Irreversible Cholinesterase Inhibitors
Very potent and toxic, irreversible cholinesterase inhibitors
Signs and symptoms are typical for cholinesterase inhibitors
Treat poisoning with atropine and pralidoxime
DFP/Isoflurophate has been used in ophthalmology for the treatment of glaucoma |
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Term
| nerve gases (*Sarin and others) |
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Definition
Irreversible Cholinesterase Inhibitors
Very potent and toxic, irreversible cholinesterase inhibitors
Signs and symptoms are typical for cholinesterase inhibitors
Treat poisoning with atropine and pralidoxime |
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Term
| pralidoxime/2-PAM (Protopam) |
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Definition
Cholinesterase Reactivator
chemically binds to the phosphate group that inhibits the enzyme and thereby regenerates the enzyme
antidote for organophosphate poisoning
must be used within 2 hours following exposure
does not work with carbamate insecticides (e.g. carbaryl) |
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Term
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Definition
Phospodiesterase-5 Inhibitors
Nitric Oxide activates guanylcyclase to produce cGMP causing vasodilation, producing erection. By inhibiting PDE-5, they prohibit it's normal breakdown of cGMP.
Peak plasma is 1 hour, Onset 30 minutes
Potential of side effects with CYP3A4 (ery, ketaconazole, cimetidine), nitrates, potentially B-blockers and a-1 blockers, sympathomimetics (cocaine). |
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Term
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Definition
Phospodiesterase-5 Inhibitors
Nitric Oxide activates guanylcyclase to produce cGMP causing vasodilation, producing erection. By inhibiting PDE-5, they prohibit it's normal breakdown of cGMP.
Peak plasma is 1 hour, Onset 30 minutes
Potential of side effects with CYP3A4 (ery, ketaconazole, cimetidine), nitrates, potentially B-blockers and a-1 blockers, sympathomimetics (cocaine). |
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Term
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Definition
Phospodiesterase-5 Inhibitors
Nitric Oxide activates guanylcyclase to produce cGMP causing vasodilation, producing erection. By inhibiting PDE-5, they prohibit it's normal breakdown of cGMP.
Longer half life and duration of action = 36 hours.
Potential of side effects with CYP3A4 (ery, ketaconazole, cimetidine), nitrates, potentially B-blockers and a-1 blockers, sympathomimetics (cocaine). |
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Term
| Botulinium Toxin (Clostridium botulinium) |
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Definition
Inhibits Release of ACh from nerve endings
Affects both autonomic (classic anticholinergic effects) and neuromuscular junction (paralysis)
Treatment involves aggressive symptomatic support and ABX to the toxin |
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Term
| atropine (AKA hyoscyamine and analogs) |
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Definition
ACh/Muscarinic Antagonists
racemic mixture of d, l-hyoscyamine. The l isomer is pharmacologically more active.
Homotropine is a semisynthetic analog of atropine |
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Term
| scopolamine (AKA hyoscine and analogs) |
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Definition
ACh/Muscarinic Antagonists
Methscopolamine is a quaternary analog that does not cross the blood-brain barrier
pharmacologic effects and uses of scopolamine are generally similar to those of atropine except it has more of a CNS depressant effect (sedation and amnesia) than atropine
prevention of motion-sickness and vertigo |
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Term
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Definition
ACh/Muscarinic Antagonists
nonquaternary antimuscarinic agent
intestinal antispasmodic for the treatment of irritable bowel syndrome |
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Term
| propantheline (Pro-Banthine) |
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Definition
ACh/Muscarinic Antagonists
antispasmodic effects (eg in the treatment of irritable bowel syndrome)
quaternary compound with few CNS effects |
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Term
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Definition
ACh/Muscarinic Antagonists
quaternary antimuscarinic agent (no CNS effects)
in anesthesiology as a preop medication to dry respiratory secretions and inhibit vagal reflexes
general purpose antimuscarinic agent |
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Term
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Definition
ACh/Muscarinic Antagonists
quaternary salt administered by inhalation for the treatment of asthma and COPD
few systemic effects |
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Term
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Definition
ACh/Muscarinic Antagonists
quaternary salt administered by inhalation for the treatment of asthma and COPD
few systemic effects
Longer duration of action |
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Term
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Definition
ACh/Muscarinic Antagonists
centrally acting antimuscarinics used in the treatment of Parkinson's disease or drug-induced Parkinsonism |
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Term
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Definition
ACh/Muscarinic Antagonists
centrally acting antimuscarinics used in the treatment of Parkinson's disease or drug-induced Parkinsonism |
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Term
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Definition
ACh/Muscarinic Antagonists
urinary incontinence due to over active bladder. |
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Term
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Definition
| ACh/Muscarinic Antagonists |
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Term
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Definition
ACh/Muscarinic Antagonists
urinary incontinence due to over active bladder. |
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Term
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Definition
ACh/Muscarinic Antagonists
used to dilate the pupil for opthamologic examination |
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Term
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Definition
ACh/Muscarinic Antagonists
urinary incontinence due to over active bladder. |
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