PHARMA Practical Revesion CNS

Download as pdf or txt
Download as pdf or txt
You are on page 1of 26

CNS Pharmacology

Practical Revision
Instructor information

§Contact: Rehab M. Elshahat


§Department: pharmacology
§Official email: rehab@azhar.edu.eg
§Mobile: 01006833432
Q1-Mention drug interaction of
phenytoin?

Q2- Write the therapeutic uses of phenytoin


Answer
Q1- Drug interaction:
-phenytoin is a potent hepatic enzyme inducer
it increase the degradation of other drugs
e.g. digitoxin , warfarin , carbamazepine,
oral contraceptives, folic acid , vit. D , vit. K
and its own.
-Hepatic enzyme inhibitors e.g.
cimetidine, chloramphenicol, isoniazid increase phenytoin plasma level.
-Hepatic enzyme inducers e.g. e.g. phenylbutazone ,rifampicin,
phenobarbitone, carbamazepine, smoking, coffee and tea.
Plasma protein:
-Some drugs displace it from pp
salicylates, phenylbutazone, Sulphonamides and valproate
displace the phenytoin from plasma protein and increase its free level.
-Other drugs phenytoin displace it from pp
thyroxin and TCA
Q3- Therapeutic uses :

1- partial and grand mal epilepsy.


it is the drug of choice with no sedation.
monitoring of plasma concentration is essential to adjust dose.
2- Status epileptics
3- Cardiac dysrhythmias.
4-teartment of trigeminal neuralgia.
Q1-List therapeutic uses of valproate?
Q2-Mention the effect of Sodium valproate, carbamazepine
and phenytoin on the fetus
Q1-List therapeutic uses of valproate?

-Therapeutic uses: Broad spectrum antiepileptic drug.


1-Absence seizures.
2-Generalized tonic -clonic seizures.
3- Myoclonic seizures (drug of choice).
4- Bipolar depressive illness.
5- Migraine headache.
6- Drug of choice in patients with mixed petit mal with grand mal
epilepsy.
Q2-Mention the effect of Sodium valproate, carbamazepine
and phenytoin on the fetus

-Antiepileptic drugs are associated with significant adverse effects and several of them
appear to affect fetal development.
Sodium valproate, carbamazepine and phenytoin are associated with an
increased risk of developing congenital abnormalities.

Sodium valproate is associated with major congenital abnormalities,


including a 20-fold increase in neural tube defects, as well as
cardiovascular abnormalities and cleft palate.
Hospital management of Status epilepticus

First-line AED : is intravenous lorazepam. If unavailable, then IV


diazepam should be administered

Second-line treatment: IV phenytoin or valproate or


phenobarbital should be administered.

In the refractory status: general anesthesia with propofol, midazolam or


thiopentone
Febrile convulsions:

The drug of choice is diazepam by IV or rectal


administration.
Prophylactic management of febrile convulsions
may be required in some children, such as those
with pre-existing risk factors or a history of
previous prolonged seizures.
Instructor information

• Contact: Sameh Ahmad Abdelghany


• Department: Clinical Pharmacology
• Official email: dr.samghany@gmail.com
• Mobile (optional): 01003798288
• Academic hours:
Ø Saturday: 10:00 AM-12:00 PM
Properties of an Ideal anaesthetic agent
For Patient:
§ Pleasant, non-irritating and should not cause nausea or vomiting
§ Induction and recovery should be fast
For Surgeon:
§ analgesia, immobility and muscle relaxation
§ nonexplosive and noninflammable
For the anaesthetist:
§ Margin of safety , Potent
§ Heart, liver and other organs
§ Cheap, stable and easily stored
§ Rapid adjustment of depth of anaesthesia
Preanesthetic medications
1) Anxiolytics(e.g diazepam):
§ given at night preoperatively to provide sedation & amnesia.
2) Opioid analgesics(e.g morphine, fentanyl,or alfentanil):
§ They are given 1½ hrs before anesthesia to inforce low potency
anesthetics as nitrous oxide.
§ Alfentanil may offer faster recovery than fentanyl.
3) Anticholinergic drugs(e.g atropine or scopolamine):
§ They are given 1½ hrs before anesthesia to reduce respiratory
secretions and prevent occurrence of aspiration pneumonia.
§ They block the reflex vagal stimulation induced by some inhalation
anesthetics.
4) Muscle relaxants (Neuromuscular blockers)
5) Others:
§ e.g. vasopressors to prevent hypotension and hypothermics
(chlorpromazine) to lower the normal body temperature in cases of
cardiac surgery.
Malignant hyperthermia
This is a rare , fatal complication of volatile liquid anesthetics.
It is genetically determined, and results from a defect in the ryanodine
receptor (RyR1) that regulates release of Ca2+ from the sarcoplasmic
reticulum in skeletal muscle cells.
A sudden increase in intracellular Ca 2+ provoked by an anaesthetic
produces:
a)-Tachycardia b)-Unstable blood pressure
c)-Hypercapnia d)-Fever and hyperventilation, followed by
e)-Hyperkalemia and metabolic acidosis.
f)-Muscle rigidity may occur.
Treatment: is with dantrolene, an RyR1 receptor antagonist .
Factors influencing the effectiveness of local anaesthetic
1) Potency of the local anaesthetic (potency is directly related to lipid
solubility).
2) The proximity of the point of injection to the nerve (operator skills).
3) The duration of the persistence of the drug at the site of application
(add a vasoconstrictor).
4) The pH of the medium:
§ A decrease in pH shifts equilibrium toward the ionized form.
§ Therefore, Inflammation increases acidity and reduces tissue buffer,
reducing the activity of local anaesthetics.
Routes of local Anesthesia
1- Topical anesthesia(spray, drops)
2- Infiltration anesthesia
3- Nerve or conduction block
4- Spinal anesthesia
5- Epidural Anesthesia
Therapeutic uses of Aspirin
1) As analgesic(for mild-moderate pain): in headache, arthritis, rheumatic
pain
2) As antipyretic: it should not be used routinely for this purpose because
fever may be a normal protective mechanism.
3) As anti-inflammatory and anti-rheumatic: in rheumatic fever, rheumatoid
arthritis, osteoarthritis, etc.
4) As antithrombotic: in ischemic heart disease
Treatment of paracetamol toxicity
1. Gastric lavage with activated charcoal.
2. Sulfhydryl donors (acetylcysteine) to restore hepatic glutathione.
It must be started within 8 hours of toxicity.
3. Haemodialysis: better within the first 12 hrs after ingestion.
Adverse effects of morphine
1. CNS:
Tolerance & physical dependence (addiction) with prolonged use.
↑↑ intracranial tension.
RC depression: the most important effect and is dose-dependent.
2. Respiratory: Bronchoconstriction.

3. CVS: Postural hypotension


4. GIT:
Nausea, vomiting, and constipation.
5. Genito-Urinary:
Urine retention especially in patients with enlarged prostate.
6. Eye: Miosis
7. Allergic reactions due to histamine release
Contraindications of morphine
1) Head injury & increased intracranial pressure
2) Respiratory depression.
3) Bronchial asthma
4) Biliary colic & gallstones
5) Senile enlarged prostate
6) Hypotension and hypovolemia
7) Hepatic damage.
8) Undiagnosed acute abdominal pain
9) Infants and old patients
Treatment of acute opioid toxicity
1) Gastric lavage.
2) Establish a patent airway and artificial respiration if needed.
3) Opioid antagonists:
§ Naloxone: pure opioid antagonist and can reverse RC depression within
minutes (0.4 - 0.8 mg i.v. for 2-3 doses).

Ø NB:
§ The duration of opioid antagonists is shorter than morphine. The patient
should be watched carefully because he may go back into coma.
§ Care should be taken to avoid withdrawal syndrome.
Treatment of chronic opioid toxicity (addiction)

1) Gradual withdrawal of morphine with substitution by methadone,


then gradual withdrawal of methadone.

2) Clonidine: to stimulate central α2 receptors and ↓ NA release.

3) Sedatives: e.g. diazepam.


26

thanks
F o r W a t c h i n g

You might also like