Cholinergic agents Flashcards
They occupy
receptor sites for ACh on the membranes of the
effector cells of the postganglionic cholinergic nerves,
causing increased stimulation of the cholinergic
recepto
Direct-acting cholinergic agonists
act at cholinergic receptors
in the peripheral nervous system to mimic the effects of ACh and
parasympathetic stimulation
The direct-acting cholinergic agonists
parasympathetic effects of direct-acting cholinergic agonists
Slowed heart
rate and decreased myocardial contractility,
Vasodilation, Bronchoconstriction and increased
bronchial mucus secretion,
Increased GI activity
and secretions, increased bladder tone,
relaxation of GI and bladder sphincters, and
pupil constriction.
These drugs usually stimulate muscarinic receptors within
the parasympathetic system.
Direct -Acting Cholinergic
Agonist
are similar to
Ach and react directly with receptor sites to cause the
same reaction as if Ach had stimulated the receptor sites.
Direct -Acting Cholinergic
Agonist
Drugs belong to this class: Direct -Acting Cholinergic
Agonist
- Bethanechol (Duvoid,
Urecholine) - Carbachol (Miostat)
- Cevimeline (Evoxac)
- pilocarpine (Pilocar, Salagen)
Contraindications Direct -Acting Cholinergic
Agonist
Patients with hypersensitivity to any component of the
drug
–Peptic ulcer, intestinal obstruction, or recent GI
surgery
-Asthma
-Bladder obstruction or impaired healing of sites from
recent bladder surgery
-Epilepsy and parkinsonism
-g pregnancy and
lactation
Drug to Drug Interaction Direct -Acting Cholinergic
Agonist
increased risk of cholinergic effects if combined or given with acetylcholinesterase
inhibitors, such as neostigmine or tacrine
These drugs work
at all ACh receptors, in the parasympathetic nervous
system, in the central nervous system (CNS), and at the
neuromuscular junction.
Indirect -Acting Cholinergic
Agonist
reversible indirect-acting cholinergic agonists fall
into two main categories:
: (1) agents used to treat
myasthenia gravis and (2) agents used to treat Alzheimer
disease.
a chronic muscular
disease caused by a defect in neuromuscular
transmission. It is thought to be an
autoimmune disease in which patients make
antibodies to their ACh receptors
Agents for Myasthenia Gravis
do not react
directly with ACh receptor sites; instead, they react
chemically with acetylcholinesterase in the synaptic cleft
to prevent it from breaking down ACh.
Indirect -Acting Cholinergic
Agonist
Drugs belong to Agents for
Myasthenia Gravis :
- Ambenonium (Mytelase)
- Edrophonium (Tensilon,
Enlon) - Neostigmine (Prostigmine)
- Pyridostigmine (Regonol,
Mestinon)
a progressive disorder
involving neural degeneration in the cortex that leads
to a marked loss of memory and of the ability to carry
on activities of daily living.
Alzheimer disease
Drugs belong toAgents for Alzheimer
Disease:
- Tacrine (Cognex)
- Galantamine (Razadyne)
- Rivastigmine (Exelon)
- Donepezil (Aricept)