NEET MDS Lessons
Pharmacology
EPHEDRINE
It act indirectly and directly on α and β receptors. It increases blood pressure both by peripheral vasoconstriction and by increasing the cardiac output. Ephedrine also relaxes the bronchial smooth muscles.
Ephedrine stimulates CNS and produces restlessness, insomnia, anxiety and tremors.
Ephedrine produces mydriasis on local as well as systemic administration.
Ephedrine is useful for the treatment of chronic and moderate type of bronchial asthma, used as nasal decongestant and as a mydriatic without cycloplegia. It is also useful in preventing ventricular asystole in Stokes Adams syndrome.
Meperidine (Demerol)
Meperidine is a phenylpiperidine and has a number of congeners. It is mostly effective in the CNS and bowel
- Produces analgesia, sedation, euphoria and respiratory depression.
- Less potent than morphine, 80-100 mg meperidine equals 10 mg morphine.
- Shorter duration of action than morphine (2-4 hrs).
- Meperidine has greater excitatory activity than does morphine and toxicity may lead to convulsions.
- Meperidine appears to have some atropine-like activity.
- Does not constrict the pupils to the same extent as morphine.
- Does not cause as much constipation as morphine.
- Spasmogenic effect on GI and biliary tract smooth muscle is less pronounced than that produced by morphine.
- Not an effective antitussive agent.
- In contrast to morphine, meperidine increases the force of oxytocin-induced contractions of the uterus.
- Often the drug of choice during delivery due to its lack of inhibitory effect on uterine contractions and its relatively short duration of action.
- It has serotonergic activity when combined with monoamine oxidase inhibitors, which can produce serotonin toxicity (clonus, hyperreflexia, hyperthermia, and agitation)
Adverse reactions to Meperidine
• Generally resemble a combination of opiate and atropine-like effects.
- respiratory depression, - tremors, - delirium and possible convulsions, - dry mouth
• The presentation of mixed symptoms (stupor and convulsions) is quite common in addicts taking large doses of meperidine.
Antidepressant Drugs
Drug treatment of depression is based on increasing serotonin (5-HT) or NE (or both) at synapses in selective tracts in the brain. This can be accomplished by different mechanisms.
Treatment takes several weeks to reach full clinical efficacy.
1. Tricyclic antidepressants (TCAs)
a. Amitriptyline
b. Desipramine
c. Doxepin
d. Imipramine
e. Protriptyline
2. Selective serotonin reuptake inhibitors (SSRIs)
a. Fluoxetine
b. Paroxetine
c. Sertraline
d. Fluvoxamine
e. Citalopram
3. Monoamine oxidase inhibitors (MAOIs)
a. Tranylcypromine
b. Phenelzine
4. Miscellaneous antidepressants
a. Bupropion
b. Maprotiline
c. Mirtazapine
d. Trazodone
e. St. John’s Wort
Antimania Drugs
These drugs are used to treat manic-depressive illness.
1. Lithium
2. Carbamazepine
3. Valproic acid
Operator position
For the right-handed operator, the 8 and 10 o’clock position and for left-handed operators, the corresponding 2 and 4 o’clock position almost always allows for optimal visualization of the injection field.
Ketamine
- Causes a dissociative anesthesia.
- Is similar to but less potent than phencyclidine.
- Induces amnesia, analgesia, catalepsy and anesthesia, but does not induce convulsions.
- The principal disadvantage of ketamine is its adverse psychic effects during emergence from anesthesia. These include: hallucinations, changes in mood and body image.
- During anesthesia, many of the protective reflexes are maintained, such as laryngeal, pharyngeal, eyelid and corneal reflexes.
- Muscle relaxation is poor.
- It is not indicated for intracranial operations because it increases cerebrospinal fluid pressure.
- Respiration is well maintained.
- Arterial blood pressure, cardiac output, and heart rate are all elevated.
Thiopental
- A barbiturate that is generally used to induce anesthesia.
- The temporal course of effects from induction to recovery depends almost entirely upon progressive redistribution.
- Metabolic degradation or excretion during anesthesia is negligible, except in the case of methohexital.
- The barbiturates produce minimal analgesia.
- Respiratory depression may be pronounced.
- Cardiac output is reduced while total peripheral resistance is increased.
- It does not sensitize the heart to catecholamines.
- It may cause bronchiospasm, especially in asthmatics.
- It is contraindicated in acute intermittent porphyria.
Sympatholytics And Alpha Adrenergic Blockers
Types
1. Alpha 1-receptor blockers: prazocin,doxazocin.
2. Centrally acting alpha 2- agonists: methyldopa, clonidine.
3. Peripherally acting adrenergic antagonists: reserpine.
4. Imidazoline receptor agonists: rilmenidine, moxonidine.
Advantages
- Alpha1- receptor blockers and imidazoline receptor agonists improve lipid profile and insulin sensitivity.
- Methyldopa: increases renal blood flow. Drug of choice during pregnancy.
- Reserpine: neutral metabolic effects and cheap.
Indications:
- Diabetes mellitus: alpha1- receptor blockers, imidazoline receptor agonists.
- Dyslipidemia: alpha 1- receptor blockers, imidazoline receptor agonists.
- Prostatic hypertrophy: alpha 1- receptor blockers.
- When there is a need for rapid reduction in blood pressure: clonidine.
Side Effects
- Prazocin: postural hypotension, diarrhea, occasional tachycardia, and tolerance (due to fluid retention).
- Methyldopa: sedation, hepatotoxicity, hemolytic anemia, and tolerance.
- Reserpine: depression, lethargy, weight loss, peptic ulcer, diarrhea, and impotence
- Clonidine: dry mouth, sedation, bradycardia, impotence, and rebound hypertension if stopped suddenly.
Considerations
- Prazocin, methyldopa, and reserpine should be combined with a diuretic because of fluid retention.
Direct Arterial Vasodilators
Types: hydralazine, diazoxide, nitroprusside, and minoxidil