NEET MDS Lessons
Pharmacology
Distribution
Three major controlling factors:
Blood Flow to Tissues: rarely a limiting factor, except in cases of abscesses and tumors.
Exiting the Vascular System: Occurs at capillary beds.
- Typical Capillary Beds - drugs pass between cells
- The Blood-Brain Barrier- Tight junctions here, so drugs must pass through cells. Must then be lipid soluble, or have transport system.
- Placenta - Does not constitute an absolute barrier to passage of drugs. Lipid soluble, nonionized compounds readily pass.
- Protein Binding: Albumin is most important plasma protein in this respect. It always remains in the blood stream, so drugs that are highly protein bound are not free to leave the bloodstream. Restricts the distribution of drugs, and can be source of drug interactions.
Entering Cells: some drugs must enter cells to reach sites of action.
Loperamide
- Similar chemically and pharmacologically to Diphenoxylate.
- Slows gastrointestinal motility by effects on the circular and longitudinal muscles of the intestine.
- Not well absorbed following oral administration.
- Useful in the treatment of diarrhea.
Isoflurane (Forane) MAC 1.3%, Blood/gas solubility ratio 1.4
- Better muscle relaxation than with the other halogenated anesthetic agents.
- Isoflurane markedly potentiates the action of the neuromuscular blocking agents.
- Produces rapid onset and recovery of anesthesia.
- Does not sensitize the heart to catecholamines.
- Produces respiratory depression, but produces less cardiovascular depression
- than does halothane.
- It has an extremely low degree of metabolism and is apparently relatively
- nontoxic.
Erythromycin
used for people who have an allergy to penicillins. For respiratory tract infections, it has better coverage of atypical organisms, including mycoplasma. It is also used to treat outbreaks of chlamydia, syphilis, and gonorrhea.
Erythromycin is produced from a strain of the actinomyces Saccaropolyspora erythraea, formerly known as Streptomyces erythraeus.
Mechanism of action Erythromycin prevents bacteria from growing, by interfering with their protein synthesis. Erythromycin binds to the subunit 50S of the bacterial ribosome, and thus inhibits the translocation of peptides.
Erythromycin is easily inactivated by gastric acids, therefore all orally administered formulations are given as either enteric coated or as more stable salts or esters. Erythromycin is very rapidly absorbed, and diffused into most tissues and phagocytes. Due to the high concentration in phagocytes, erythromycin is actively transported to the site of infection, where during active phagocytosis, large concentrations of erythromycin are released.
Most of erythromycin is metabolised by demethylation in the liver. Its main route elimination route is in the bile, and a small portion in the urine.
Erythromycin's half-life is 1.5 hours.
Side-effects. More serious side-effects, such as reversible deafness are rare. Cholestatic jaundice, Stevens-Johnson syndrome and toxic epidermal necrosis are some other rare side effects that may occur.
Contraindications Earlier case reports on sudden death prompted a study on a large cohort that confirmed a link between erythromycin, ventricular tachycardia and sudden cardiac death in patients also taking drugs that prolong the metabolism of erythromycin (like verapamil or diltiazem)
erythromycin should not be administered in patients using these drugs, or drugs that also prolong the QT time.
Ofloxacin : It is a quinolone antibiotic and similar in structure to levofloxacin. It is an alternative treatment to ciprofloxacin for anthrax.
Topical Anesthetics
Benzocaine
Benzocaine is a derivative of procaine, an ester type local anesthetic, and is poorly soluble in water and is
available only as a topical anesthetic.
- Localized allergic reactions are sometimes encountered
- Overdosing is unlikely as benzocaine is poorly absorbed into the blood, which decreases the likelihood of systemic toxicity.
- The onset of surface anesthesia is rapid requiring less than one minute.
Tetracaine
- Tetracaine is an ester type local anesthetic
- Topically applied tetracaine as opposed to benzocaine has a prolonged duration of action.
Cocaine
- Cocaine is a ester type anesthetic that is used exclusively as a topical agent.
- Cocaine is unique among topical and injectable anesthetics in that it has vasoconstrictive as well as anesthetic properties. It is used sparingly because of its abuse potential but is still used when hemostasis of mucous membranes is essential.
- Cocaine is generally available in concentrations of 2-10 % solution.
Lidocaine
- Lidocaine is an amide local anesthetic that is available in injectable and topical formulations.
- It is available in gel, viscous solution, ointment and aerosol preparations in concentrations ranging from 2-10 %.
- The onset of anesthesia is slower relative to benzocaine but, the duration is about the same.
- Absorption into the bloodstream is greater than benzocaine providing a greater risk of systemic toxicity.
Gastric acid neutralizers (antacids)
Antacids act primarily in the stomach and are used to prevent and treat peptic ulcer. They are also used in the treatment of Reflux esophagitis and Gastritis.
Mechanism of action:
Antacids are alkaline substances (weak bases) that neutralize gastric acid (hydrochloric acid) they react with hydrochloric acid in the stomach to produce neutral or less acidic or poorly absorbed products and raise the pH of stomach secretion.
Antacids are divided into systemic and non-systemic.
• Systemic antacids (e.g. sodium bicarbonate) are highly absorbed into systemic circulation and enter body fluids. Therefore, they may alter acid–base balance. They can be used in the treatment of metabolic acidosis.
Non-systemic: they do not alter acid–base balance significantly, because they are not well-absorbed into the systemic circulation. They are used as gastric antacids; and include:
• Magnesium compounds such as magnesium hydroxide and magnesium sulphate MgS2O3. They have relatively high neutralizing capacity, rapid onset of action, however, they may cause diarrhoea and hypermagnesemia.
• Aluminium compounds such as aluminium hydroxide. Generally, these have low neutralizing capacity, slow onset of action but long duration of action. They may cause constipation.
• Calcium compounds such as. These are highly effective and have a rapid onset of action but may cause hypersecretion of acid (acid - rebound) and milk-alkali syndrome (hence rarely used in peptic ulcer disease).
Therefore, the most commonly used antacids are mixtures of aluminium hydroxide and magnesium hydroxide .