NEET MDS Lessons
Pharmacology
Mixed Narcotic Agonists/Antagonists
These drugs all produce analgesia, but have a lower potential for abuse and do not produce as much respiratory depression.
A. Pentazocine
- Has a combination of opiate analgesic and antagonist activity.
- Orally, it has about the same analgesic potency as codeine.
- In contrast to morphine, cardiac workload tends to increase due to an increase in pulmonary arterial and cerebrovascular pressure. Blood pressure and heart rate both also tend to increase.
- Adverse reactions to Pentazocine
• Nausea, vomiting, dizziness.
• Psychotomimetic effects, such as dysphoria, nightmares and visual hallucinations.
• Constipation is less marked than with morphine.
B. Nalbuphine
- Has both analgesic and antagonist properties.
- Resembles pentazocine pharmacologically.
- Analgesic potency approximately the same as morphine.
- Appears to be less hypotensive than morphine.
- Respiratory depression similar to morphine, but appears to peak-out at higher doses and to reach a ceiling.
- Like morphine, nalbuphine reduces myocardial oxygen demand. May be of value following acute myocardial infarction due to both its analgesic properties and reduced myocardial oxygen demand.
- Most frequent side effect is sedation.
C. Butorphanol
- Has both opiate agonist and antagonist properties.Resembles pentazocine , pharmacologically., 3.5 to 7 times more potent than morphine., Produces respiratory depression, but this effect peaks out with higher doses. The respiratory depression that does occur lasts longer than that seen following morphine administration.
- Butorphanol, like pentazocine, increases pulmonary arterial pressure and possibly the workload on the heart.
- Adverse reactions include sedation, nausea and sweating.
D. Buprenorphine
- A derivative of eto`rphine. Has both agonist and antagonist activity. 20 to 30 times more potent than morphine.Duration of action only slightly longer than morphine, but respiratory depression and miosis persist well after analgesia has disappeared.
- Respiratory depression reaches a ceiling at relatively low doses.
- Approximately 96% of the circulating drug is bound to plasma proteins.
- Side effects are similar to other opiates:
- sedation, nausea, vomiting,
- dizziness, sweating and headache.
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
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.
Antiplatelet Drugs:
Whereas the anticoagulant drugs such as Warfarin and Heparin suppress the synthesis or activity of the clotting factors and are used to control venous thromboembolic disorders, the antithrombotic drugs suppress platelet function and are used primarily for arterial thrombotic disease. Platelet plugs form the bulk of arterial thrombi.
Acetylsalicylic acid (Aspirin)
• Inhibits release of ADP by platelets and their aggregation by acetylating the enzymes (cyclooxygenases or COX) of the platelet that synthesize the precursors of Thromboxane A2 that is a labile inducer of platelet aggregation and a potent vasoconstrictor.
• Low dose (160-320 mg) may be more effective in inhibiting Thromboxane A2 than PGI2 which has the opposite effect and is synthesized by the endothelium.
• The effect of aspirin is irreversible.
Ciprofloxacin : Ciprofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase
Ciprofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
Enterobacteriaceae, Vibrio, Hemophilus influenzae, Neisseria gonorrhoeae
Neisseria menigitidis, Moraxella catarrhalis, Brucella, Campylobacter,
Mycobacterium intracellulare, Legionella sp., Pseudomonas aeruginosa,
Bacillus anthracis - that causes anthrax
Weak activity against: Streptococcus pneumoniae,
No activity against: Bacteroides, Enterococcus faecium, Ureaplasma urealyticum and others
It is contraindicated in children, pregnancy, and epilepsy.
Ciprofloxacin can cause photosensitivity reactions and can elevate plasma
theophylline levels to toxic values. It can also cause constipation and sensitivity to caffeine.
Dosage in respiratory infections is 500-1500 mg a day in 2 doses.
Carbonic anhydrase inhibitors
Acetazolamide, Dichlorphenamide, Methazolamide, Ethoxzolamide
Mechanism of Action
1. Carbonic anhydrase (CA) facilitates excretion of H+ and recovery of bicarbonate by the proximal renal tubule and ciliary epithelium of the eye. Sodium is recovered in exchange for H+.
2. Inhibitors block CA block sodium recovery. A very mild diuresis is produced (this is really a side effect of their use in glaucoma) because relatively unimportant mechanism for Na recovery and because proximal tubule site means that other sodium recovery mechansims continue to process their normal fraction of the sodium load.
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