NEET MDS Lessons
Pharmacology
Dissociation constants
|
Local anesthetic |
pKa |
% of base(RN) at pH 7.4 |
onset of action(min) |
|
Lidocaine |
7.8 |
29 |
2-4 |
|
Bupivacaine |
8.1 |
17 |
5-8 |
|
Mepivacaine |
7.7 |
33 |
2-4 |
|
Prilocaine |
7.9 |
25 |
2-4 |
|
Articaine |
7.8 |
29 |
2-4 |
|
Procaine |
9.1 |
2 |
14-18 |
|
Benzocaine |
3.5 |
100 |
- |
Codeine
Codeine is methyl morphine, with a methyl substitution on the phenolic hydroxyl group of morphine. It is more lipophilic than morphine and thus crosses the blood–brain barrier faster.
- classified as a simple, or mild analgesic, codeine is often used in low doses as an oral analgesic has a much better oral/parenteral absorption ratio than morphine.
- Effective for mild to moderate pain.
- Constipation occurs
- Dizziness may occur in ambulatory patients.
- More potent histamine-releasing action than does morphine.
- Should not be administered by IV injection.
- Extremely effective antitussive agent and is used therapeutically for suppressing cough.
- In contrast to morphine, codeine overdose can occasionally lead to the production of seizures.
- Seizures can be treated with barbiturates.
- Respiratory depression can be counteracted with Naloxone.
- orally, 30 mg of codeine is equi-analgesic to 600 mg of aspirin, however, the effects of the two are additive, and occasionally synergistic
Nitrous Oxide (N2O)
MAC 100%, blood/gas solubility ratio 0.47
- An inorganic gas., low solubility in blood, but greater solubility than N2
- Inflammable, but does support combustion.
- Excreted primarily unchanged through the lungs.
- It provides amnesia and analgesia when administered alone.
- Does not produce muscular relaxation.
- Less depressant to both the cardiovascular system and respiratory system than most of the other inhalational anesthetics.
- Lack of potency and tendency to produce anoxia are its primary limitations.
- The major benefit of nitrous oxide is its ability to reduce the amount of the secondary anesthetic agent that is necessary to reach a specified level of anesthesia.
Antianginal Drugs
Organic Nitrates :
Short acting: Glyceryl trinitrate (Nitroglycerine, GTN), Amyl Nitrate
Long Acting: Isosrbide dinitrate (Short acting by sublingual route), Erythrityl tetranitrate, penta erythrityl tetranitrate
Beta-adrenergic blocking agents : Propanolol, Metoprolol
Calcium channel blockers Verapamil, Nifedipine, Dipyridamole
Mechanism of action
– Decrease myocardial demand
– increase blood supply to the myocardium
Helicobacter Pylori Agents
Antimicrobial
• Amoxicillin,
• Clarithromycin,
• Metronidozole
• Tetracycline
Antisecreteory agents accelerates symptom relief and yield healing (omeprozole)
Bismuth subsalicylate
Therapy For H. Pylori
Original
• Tetracycline
• Metronidazole (Flagyl)
• Bismuth subsalicylate
• Given for 14 days
• >90% effective in eradicating microorganisms
New triple therapy
• Amoxicillin
• Clarithromycin
• Omeprazole (Prilosec)
• Given for 7 days
• >90% effective in eradicating microorganisms
Dual Therapy
Amoxicillin or clarithromycin
Omeprazole
Given for 14 days
60-80% effective in eradication of H. Pylori
Antimania Drugs
MANIC SYMPTOMSMANIC SYMPTOMS
Elevated or irritable mood
Increased activity or psychomotor agitation
Reduced need for sleep
Inflated self esteem or grandiosity
Increased or pressure of speech
Flight of ideas
These drugs are used to treat manic-depressive illness.
1. Lithium
2. Carbamazepine
3. Valproic acid
Mechanisms of action
1. Lithium works inside the cell to block conversion of inositol phosphate to inositol.
2. Carbamazepine blocks sodium channels
3. Valproic acid blocks sodium and calcium channels
PHARMACOKINETICS
Absorbed readily and almost completely from the GI tract; peak concentrations in 1-2 hrs
Lithium toxicity
1. Nausea, diarrhea, convulsions, coma, hyperreflexia, cardiac arrhythmias, hypotension.
2. Thyroid enlargement; increases thyroid stimulating hormone (TSH) secretion; may cause hypothyroidism.
3. Polydipsia, polyuria (lithium inhibits the effect of antidiuretic hormone on the kidney).
Clinical applications concerning lithium
- Patients must be warned against sodium-restricted diets because sodium restriction leads to greater retention of lithium by the kidney.
- Patients must have regular (e.g., monthly) blood checks because the margin of safety is narrow.
Endocrine Effects – Goitre and hypothyroidism commonly
Cardiac Effects:– ECG changes(common) - T-wave flattening/inversion and appearance of U wavesflattening/inversion and appearance of U waves
Li and Pregnancy -1st Trimester:Cardiovascular anomalies of the newborn, especially Ebstein's malformation
- 3rd Trimester: Neonatal goiter, CNS depression, hypotonia ("floppy baby" syndrome)
Drug–drug interactions of lithium
Diuretics and newer nonsteroidal anti-inflammatory drugs (NSAIDs) reduce lithium excretion and may cause lithium toxicity.
Doxycycline
Commonly prescribed for infections and to treat acne. treat urinary tract infections, gum disease, and other bacterial infections such as gonorrhea and chlamydia., as a prophylactic treatment for infection by Bacillus anthracis (anthrax). It is also effective against Yersinia pestis and malaria.