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Transmission in CNS
A nerve impulse (electric current) passé along axon to presynaptic membrane.
Release neurotransmitter into synaptic cleft. NT interacts with receptors on effector cells to
induce response.
NT released in response to action potentials is voltage dependent & require calcium influx
(Neuroregulators).
Transmission in C.N.S.
A- Release of Excitatory transmitter by Neuron (1) Cause depolarization of postsynaptic
membrane of neuron
(2) Cause Conduction of N impulse [postsynaptic excitation].
B- Release of Inhibitory Transmitter by Neuron Cause Hyper polarization of postsynaptic
membrane .
(2) Block conduction of nerve impulse [postsynaptic inhibition]
Neurotransmitters can be classified into:
1. Amino acids: Excitatory A.A. : Glutamate & Aspartate
Inhibitory A.A. : GABA & Glycine.
3. Monoamines : Noradrenaline , Adrenaline , Dopamine, 5-HT
4- Choline ester: Acetylcholine
gamma amino butyric acid (GABA)
Major inhibitory transmitter at all levels of brain GABA is a ligand gated cl- ion channel. Stimulation
of GABA receptors cause change in postsynaptic membrane permeability to become permeable
to chloride (cl-) results in hyperpolarization of the receptive neuron. Benzodiazepines,
Barbiturates, Sod. Valporate
, Ivermectin , increase binding GABA to Rs
CNs stimulants
1-Cerebral stimulants
Xanthines (Caffeine, Theophylline & Theo bromine), Amphetamine. Stimtimulate motor & sensory
area so elevated physical & mental a Wakefulness, refreshment,
Caffeine (coffee seeds), theophylline (tea leaves) , Theo bromine (coca seeds) & methylated
Xanthine.
MOA: Caffeine Inhibit Phosphodiesterase enz.
so c-AM P in cerebral cortex neurons.
Pharmacological effects
• 1.Stimulates CNS, decrease fatigue and increases motor activity. 2.Stimulate the heart and causes
vasodilation. 3.Relaxation of smooth muscle therefore theophylline is used in asthma. 4.Diuretic
effect through increasing renal blood flow. 5.Stimulation of gastric acid secretion.
Amphetamine
• Mechanism of action It increases the release of Norepinephrine and Dopamine from the nerve
endings leading to CNS stimulation
2-Medullary Stimulants
• Doxapram Mechanism of action It stimulates the respiratory center in the medulla and causes
respiratory stimulation. Clinical uses 1.Antagonizes the respiratory depressant action of
Barbiturates. 2.Antagonizes the sedative action of xylazine.
Pentylenetetrazole
• It is a respiratory stimulant. It increases respiration. High doses produce convulsion and it is used as
respiratory stimulant. 4aminopyridine It is used as respiratory stimulant and antagonizes the
sedative effect of xylazine. Nikethamide It is a short acting respiratory stimulant.
Sedatives and Hypnotics
Hypnotics are drugs that cause hypnosis by depressing the CNS so the animal is less
responsive to external stimuli. Hypnotics that used in small doses will cause sedation.
Types Barbiturates Divided into: A.Long acting (Phenobarbital)
B.Short acting (Pentobarbital) C.
Ultrashort acting (Thiopental)
Mechanism of action Potentiate the effect of GABA neurotransmitter leading to
depression of the brain and inhibits excessive motor discharge
Pharmacological effects
1.Depresses all functions of the brain. 2.Selectively depresses the motor cortex.
3.Depresses the respiratory center in medulla. 4.Produce good muscle relaxation.
5.Decreases blood pressure and heart rate. 6.Induce microsomal enzymes and
increase the metabolic rate of the animal.
Clinical uses 1.Sedative. 2.Hypnotic. 3.Anticonvulsant. 4.Anesthetics.
Benzodiazepines Which include long acting diazepam and chlordiazepoxide(2-3 day) ,
intermediate (10-20 h)alprazolam and
Mechanism of action Increasing the action of GABA neurotransmitter on its receptor
which causes influx of chloride ion into the neuronal cells leading to depression of
the CNS.
Clinical uses 1.Sedative. 2.Hypnotic. 3.Muscle relaxant. 4.Anticonvulsant.
5.Preanesthetic. 6.Antianxiety.
Chloralhydrate It is hypnotic given I.V . in large animals (7%). It depresses the
respiratory and vasomotor centers. It is metabolized in the body by reduction into
Trichloroethanol which is the active metabolite responsible of hypnotic effect of
chloral hydrate. It is used as anesthetic in equine species with weak analgesic effect
and can be mixed with Magnesium sulfate (MgSO4) (6%) to produce muscle
relaxation. Chloral hydrate decreases blood pressure and decreases heart rate
and sudden death may occur in horses which are highly excited.
Ethanol It has sedative effect, depresses respiration and causes vasodilation. It has
diuretic effect because it inhibits antidiuretic hormone (ADH). It metabolized into
CO2 and H2O and small amount expired by the lungs
Anticonvulsant Drugs
Anticonvulsant Drugs Are drugs used to control seizure through depressing the CNS.
Types Barbiturates Benzodiazepines Phenytoin Mechanism of action It stabilizes
the neuronal membranes and selectively depresses the motor areas in the brain. It
is not hypnotic.
Primidone
The structure of this drug and its mechanism of action is similar to phenobarbital and
about 25 % of the drug is metabolized into phenobarbital.
Narcotic Analgesics
Are drugs used to produce analgesia through its action on the CNS. Opioids agonists
Types 1.Natural like Morphine. 2.Synthetic like Fentanyl.
Morphine Mechanism of action It acts on opioid receptor (Mu receptor) in the CNS
leading to depression of the brain and causing analgesia.
Pharmacological effects A. On the brain:
1. Produces analgesia by increasing the pain threshold.
3.Produces euphoria in human. 4.Stimulates the Chemoreceptor Trigger Zone (CTZ) in
the brain leading to emesis in dogs. 5.Depresses the cough center. 6.Depresses the
respiratory center in the brain.
Activation of the opioid receptor decreases Ca2+ influx in response to incoming action
potential. This decreases release of excitatory neurotransmitters, such as
glutamate.
Clinical uses -Analgesic. -Preanesthetic.
Toxicity Death may result from respiratory depression and it can be treated by giving
opioid receptor antagonist like Naloxone.
Tranquilizers
Are drugs used to tranquilize and control of the animals and they are called also
Neuroleptics. Phenothiazine derivatives Types Chlorpromazine, Acepromazine and
Promazine.
Chlorpromazine Mechanism of action They antagonize dopamine receptors in the brain
leading to depression of the CNS. It also has anticholinergic and antiadrenergic
effects.
Clinical uses 1.Control the nervous animals. 2.Preanesthetic. 3.Antipruritus.
4.Antiemetic. 5.Antistress in transporting of animals. Side effects 1.Incoordination in
horses. 2.Dry mouth. 3.Constipation. 4.Hypotension. 5.Decreases body
temperature.
central nervous system

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central nervous system

  • 1.
  • 2. Transmission in CNS A nerve impulse (electric current) passé along axon to presynaptic membrane. Release neurotransmitter into synaptic cleft. NT interacts with receptors on effector cells to induce response. NT released in response to action potentials is voltage dependent & require calcium influx (Neuroregulators). Transmission in C.N.S. A- Release of Excitatory transmitter by Neuron (1) Cause depolarization of postsynaptic membrane of neuron (2) Cause Conduction of N impulse [postsynaptic excitation]. B- Release of Inhibitory Transmitter by Neuron Cause Hyper polarization of postsynaptic membrane . (2) Block conduction of nerve impulse [postsynaptic inhibition]
  • 3.
  • 4. Neurotransmitters can be classified into: 1. Amino acids: Excitatory A.A. : Glutamate & Aspartate Inhibitory A.A. : GABA & Glycine. 3. Monoamines : Noradrenaline , Adrenaline , Dopamine, 5-HT 4- Choline ester: Acetylcholine gamma amino butyric acid (GABA) Major inhibitory transmitter at all levels of brain GABA is a ligand gated cl- ion channel. Stimulation of GABA receptors cause change in postsynaptic membrane permeability to become permeable to chloride (cl-) results in hyperpolarization of the receptive neuron. Benzodiazepines, Barbiturates, Sod. Valporate , Ivermectin , increase binding GABA to Rs CNs stimulants 1-Cerebral stimulants Xanthines (Caffeine, Theophylline & Theo bromine), Amphetamine. Stimtimulate motor & sensory area so elevated physical & mental a Wakefulness, refreshment, Caffeine (coffee seeds), theophylline (tea leaves) , Theo bromine (coca seeds) & methylated Xanthine. MOA: Caffeine Inhibit Phosphodiesterase enz. so c-AM P in cerebral cortex neurons. Pharmacological effects • 1.Stimulates CNS, decrease fatigue and increases motor activity. 2.Stimulate the heart and causes vasodilation. 3.Relaxation of smooth muscle therefore theophylline is used in asthma. 4.Diuretic effect through increasing renal blood flow. 5.Stimulation of gastric acid secretion. Amphetamine • Mechanism of action It increases the release of Norepinephrine and Dopamine from the nerve endings leading to CNS stimulation 2-Medullary Stimulants
  • 5. • Doxapram Mechanism of action It stimulates the respiratory center in the medulla and causes respiratory stimulation. Clinical uses 1.Antagonizes the respiratory depressant action of Barbiturates. 2.Antagonizes the sedative action of xylazine. Pentylenetetrazole • It is a respiratory stimulant. It increases respiration. High doses produce convulsion and it is used as respiratory stimulant. 4aminopyridine It is used as respiratory stimulant and antagonizes the sedative effect of xylazine. Nikethamide It is a short acting respiratory stimulant. Sedatives and Hypnotics Hypnotics are drugs that cause hypnosis by depressing the CNS so the animal is less responsive to external stimuli. Hypnotics that used in small doses will cause sedation. Types Barbiturates Divided into: A.Long acting (Phenobarbital) B.Short acting (Pentobarbital) C. Ultrashort acting (Thiopental) Mechanism of action Potentiate the effect of GABA neurotransmitter leading to depression of the brain and inhibits excessive motor discharge Pharmacological effects
  • 6. 1.Depresses all functions of the brain. 2.Selectively depresses the motor cortex. 3.Depresses the respiratory center in medulla. 4.Produce good muscle relaxation. 5.Decreases blood pressure and heart rate. 6.Induce microsomal enzymes and increase the metabolic rate of the animal. Clinical uses 1.Sedative. 2.Hypnotic. 3.Anticonvulsant. 4.Anesthetics. Benzodiazepines Which include long acting diazepam and chlordiazepoxide(2-3 day) , intermediate (10-20 h)alprazolam and Mechanism of action Increasing the action of GABA neurotransmitter on its receptor which causes influx of chloride ion into the neuronal cells leading to depression of the CNS. Clinical uses 1.Sedative. 2.Hypnotic. 3.Muscle relaxant. 4.Anticonvulsant. 5.Preanesthetic. 6.Antianxiety. Chloralhydrate It is hypnotic given I.V . in large animals (7%). It depresses the respiratory and vasomotor centers. It is metabolized in the body by reduction into Trichloroethanol which is the active metabolite responsible of hypnotic effect of chloral hydrate. It is used as anesthetic in equine species with weak analgesic effect and can be mixed with Magnesium sulfate (MgSO4) (6%) to produce muscle
  • 7. relaxation. Chloral hydrate decreases blood pressure and decreases heart rate and sudden death may occur in horses which are highly excited. Ethanol It has sedative effect, depresses respiration and causes vasodilation. It has diuretic effect because it inhibits antidiuretic hormone (ADH). It metabolized into CO2 and H2O and small amount expired by the lungs Anticonvulsant Drugs Anticonvulsant Drugs Are drugs used to control seizure through depressing the CNS. Types Barbiturates Benzodiazepines Phenytoin Mechanism of action It stabilizes the neuronal membranes and selectively depresses the motor areas in the brain. It is not hypnotic. Primidone The structure of this drug and its mechanism of action is similar to phenobarbital and about 25 % of the drug is metabolized into phenobarbital. Narcotic Analgesics Are drugs used to produce analgesia through its action on the CNS. Opioids agonists Types 1.Natural like Morphine. 2.Synthetic like Fentanyl.
  • 8. Morphine Mechanism of action It acts on opioid receptor (Mu receptor) in the CNS leading to depression of the brain and causing analgesia. Pharmacological effects A. On the brain: 1. Produces analgesia by increasing the pain threshold. 3.Produces euphoria in human. 4.Stimulates the Chemoreceptor Trigger Zone (CTZ) in the brain leading to emesis in dogs. 5.Depresses the cough center. 6.Depresses the respiratory center in the brain. Activation of the opioid receptor decreases Ca2+ influx in response to incoming action potential. This decreases release of excitatory neurotransmitters, such as glutamate.
  • 9.
  • 10. Clinical uses -Analgesic. -Preanesthetic. Toxicity Death may result from respiratory depression and it can be treated by giving opioid receptor antagonist like Naloxone. Tranquilizers Are drugs used to tranquilize and control of the animals and they are called also Neuroleptics. Phenothiazine derivatives Types Chlorpromazine, Acepromazine and Promazine. Chlorpromazine Mechanism of action They antagonize dopamine receptors in the brain leading to depression of the CNS. It also has anticholinergic and antiadrenergic effects. Clinical uses 1.Control the nervous animals. 2.Preanesthetic. 3.Antipruritus. 4.Antiemetic. 5.Antistress in transporting of animals. Side effects 1.Incoordination in horses. 2.Dry mouth. 3.Constipation. 4.Hypotension. 5.Decreases body temperature.