- •Simplicified version! Drugs Affecting the Afferent Innervation
- •Indications:
- •Indications 3 - 6
- •Indication 1
- •Indication 2
- •Indications:
- •(CholinOnegative drugs)
- •Anticholinesterases
- •Muscarinic agonists (m-cholinomimetics)
- •Nicotinic agonists (n-cholinomimetics)
- •Simplicified version
- •(Cholinonegative drugs)
- •Muscarinic antagonists (m-cholinoblockers)
- •Nicotinic antagonists (n-cholinoblockers)
- •Ganglion-blocking drugs
- •Neuromuscular blocking drugs (myorelaxants)
- •Simplicified version
- •(Adrenopositive drugs)
- •Indirect adrenomimetics
- •Direct adrenomimetics
- •Mixed action Adrenomimetics
- •Alfa-adrenomimetics
- •Beta-adrenomimetics
- •Simplicified version
- •(Adrenonegative drugs)
- •Sympatholytics
- •Alfa-adrenoblockers
- •Beta-adrenoblockers
- •General anesthetics
- •Analgesic drugs
- •Hypnotic drugs
- •Antiepileptic drugs (anticonvulsants)
- •Sedative drugs
- •Anxyolytics (antianxiety drugs, tranquillizers)
- •Antipsychotic drugs (neuroleptics)
- •Analeptics
This effect is carried out by the reflex way because the definite
skin areas are connected with definite inner organs through the
corresponding segments of the spinal cord.
Effect in the site of drug application: - vasodilation (with hyperemia of
skin etc.) - vasoconstriction (with whiteness
of skin etc.)
Indications 3 - 6
Indication 1
Indication 2
Indications:
1/ Prophylaxy of bedsore: camphor, turpentine oil, ammonium liniment (main effect – prevention of pus inflammation due to local intensification of blood circulation; apply onto the skin with risk of bedsore formation).
2. Rhinitis: menthol (main effect – decreasing of running nose due to vasoconstriction; apply by drops in the nose).
3. Joint pain, neuralgia, myositis: camphor, turpentine oil, ammonium liniment (main effect – decreasing of pain; apply onto the skin above the injured joint, nerve or muscle).
4. Respiratory organs diseases, for example pneumonia, bronchitis: camphor, turpentine oil, ammonium liniment (main effect – decreasing of inflammation; apply onto the skin of the back)
5. Stenocardia (angina pectoris): validolum (main effect – decreasing of cardiac pain due to relaxation of coronary arteries and increasing of blood supply to the heart).
6. Fainting (syncope): ammonium solution (main effect – restoration of consciousness; give it to breath in for patient during syncope).
Some aspects of physiology. VERY IMPORTANT!!!
Cholinergic synapses (most of them are parasympathetic synapses), as any another synapses in the organism, consist of two parts: presynaps and postsynaps. Presynaps releases acetylcholine, which activates Muscarinic (M) or Nicotinic (N) cholinoreceptors on the postsynaptic membrane. Thereafter acetylcholine is destroyed by specific enzyme – acetylcholinesterase, which is located on the postsynaptic membrane.
Acetylcholine produces next effects (see and study the table):
Type of receptors |
Organ |
Effect |
Stimulation of M-cholinoreceptors |
Eye |
Constriction of pupil (miosis) |
Salivary glands |
Increasing of saliva secretion |
|
Heart |
Decreasing of heart rate, heart contractility, heart conductance and heart excitability |
|
Bronchi |
Constriction (due to contraction of smooth muscles of bronchi) |
|
Gastro-intestinal tract (GIT) organs: stomach, small intestine, gall bladder etc. |
Increasing of motility (due to contraction of smooth muscles of GIT organs) |
|
Urinary bladder |
Constriction (due to contraction of smooth muscles of urinary bladder) |
|
Stimulation of N-cholinoreceptors |
Skeletal muscles |
Increasing of contractility |
Autonomic ganglions |
Constriction of blood vessels Increasing of uterus contractility |
(CholinOnegative drugs)
Anticholinesterases
List of drugs
Reversible anticholinesterases: Neostigmine bromide, Pyridostigmine bromide
Irreversible anticholinesterases: Arminum, Echothiophate
Mechanism of action
These drugs produce inhibition of acetylcholinesterase that results in accumulation of acetylcholine in the synaptic cleft.
Neostigmine and pyridostigmine produce reversible inhibition of acetylcholinesterase, arminum and echothiophate produce irreversible inhibition of acetylcholinesterase
Pharmacological effects
These drugs produce inhibition of acetylcholinesterase that results in accumulation of acetylcholine in the synaptic cleft. In this situation acetylcholine more stronger activates M- and N-cholinergic receptors and, therefore, induces aforementioned effects:
Type of receptors |
Organ |
Effect |
Stimulation of M-cholinoreceptors |
Eye |
Constriction of pupil (miosis) |
Salivary glands |
Increasing of saliva secretion |
|
Heart |
Decreasing of heart rate, heart contractility, heart conductance and heart excitability |
|
Bronchi |
Constriction (due to contraction of smooth muscles of bronchi) |
|
Gastro-intestinal tract (GIT) organs: stomach, small intestine, gall bladder etc. |
Increasing of motility (due to contraction of smooth muscles of GIT organs) |
|
Urinary bladder |
Constriction (due to contraction of smooth muscles of urinary bladder) |
|
Stimulation of N-cholinoreceptors |
Skeletal muscles |
Increasing of contractility |
Autonomic ganglions |
Constriction of blood vessels Increasing of uterus contractility |
Indications
1. Glaucoma (increasing of intraocular pressure)
Neostigmine, Pyridostigmine, Arminum, Echothiophate → constriction of pupil → decreasing of intraocular pressure → treating of glaucoma. This effect depends on M-cholinoreceptors.
2. Atony of GIT organs and urinary bladder
Neostigmine, Pyridostigmine → increasing of motility of GIT organs and urinary bladder → treating of atony. This effect depends on M-cholinoreceptors.
3. Poor uterine contraction strength
Neostigmine, Pyridostigmine → increasing of uterus contractility → inducing of labor (delivery).
This effect depends on N-cholinoreceptors.
4. Myasthenia gravis (weakness of skeletal muscles)
Neostigmine, Pyridostigmine → increasing of contractility of skeletal muscles → treating of myasthenia gravis This effect depends on N-cholinoreceptors.