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Pharmacology - NEETMDS- courses
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Pharmacology

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.

Carbamazepine (Tegretol): most common; for generalized tonic-clonic and all partial seizures; especially active in temporal lobe epilepsies

Mechanism: ↓ reactivation of Na channels (↑ refractory period, blocks high frequency cell firing, ↓ seizure spread)

Side effects: induces hepatic microsomal enzymes (can enhance metabolism of other drugs)

Pharmacology is the study of drugs and the way they interact with living systems.  Clinical pharmacology is the study of drugs in humans.

A drug is any chemical that can effect living processes.

Therapeutics: the medical use of drugs.

An ideal drug has several important properties.  Three of these properties are of utmost importance: effectiveness, safety and selectivity. 

Effectiveness: This is the most important quality that a drug can have.  Effectiveness refers to the drug's ability to do what it is supposed to do.

Safety:  Although no drug can be totally safe, proper usage can lessen the risks of adverse effects.

Selectivity:  A truly selective drug would have no side effects, and would effect only the body process' for which it is designed and given.  Therefore, there is no such thing as a selective drug.

Pharmacokinetics: The way the body deals with a drug.  Pharmacokinetics is concerned with the processes of absorption, distribution, metabolism and excretion.

Pharmacodynamics:  What a drug does to the body.

Pharmacokinetics and pharmacodynamics are two of the processes that determine how a person will respond to a drug.  Other factors include how a drug is administered (dose, route, and timing of administration), interactions with other drugs, and individual physiological variables (weight, age, function of body systems).

Phenoxymethylpenicillin (penicillin V) Phenoxymethylpenicillin, commonly known as penicillin V, is the orally-active form of penicillin. It is less active than benzylpenicillin

Indications:

infections caused by Streptococcus pyogenes, tonsillitis, pharyngitis, skin infections, prophylaxis of rheumatic fever, moderate-to-severe gingivitis (with metronidazole)

Dental implications of these drugs: 


1.    Adverse effects: gingival hyperplasia (phenytoin), osteomalacia (phenytoin, Phenobarbital), blood dyscrasias (all but rare)
2.    Drug interactions: additive CNS depression (anesthetics, anxiolytics, opioid analgesics), induction of hepatic microsomal enzymes (phenytoin, Phenobarbital, carbamazepine), plasma protein binding (phenytoin and valproic acid)
3.    Seizure susceptibility: stress can → seizures

Selective serotonin reuptake inhibitors (SSRIs)

e.g. fluoxetine, paroxetine, citalopram, and sertraline
- Most commonly used antidepressant category
- Less likely to cause anticholinergic side effects
- Relatively safest antidepressant group in overdose
- Selectively inhibits reuptake of serotonin(5-HT)

Mode of Action;
- Well absorbed when given orally
- Plasma half-lives of 18-24 h allowing once daily dosagedaily dosage
- Metabolised through CYP450 system and most SSRIs inhibit some CYP isoforms
- Therapeutic effect is delayed for 2-4 weeks

ADVERSE DRUG REACTIONS

- Insomnia, increased anxiety, irritability
- Decreased libido
- Erectile dysfunction, anorgasmia, and ejaculatory delay
- Bleeding disorders
- Withdrawal syndrome

Balanced Anesthesia
A barbiturate, narcotic analgesic agent, neuromuscular blocking agent, nitrous oxide and one of the more potent inhalation anesthetic.

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