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Pharmacology

Hydromorphone

  • About 8-10 times more potent than morphine when given intravenously.
  • Slightly shorter duration of action.
  • More soluble than morphine, thus higher concentrations may be injected if necessary.
  • Better oral/parenteral absorption ratio than morphine, but not as good as codeine or oxycodone.
  • It is used for the treatment of moderate to severe pain

Routes of Drug Administration

Intravenous

  • No barriers to absorption since drug is put directly into the blood.
  • There is a very rapid onset for drugs administered intravenously.  This can be advantagous in emergency situations, but can also be very dangerous.
  • This route offers a great deal of control in respect to drug levels in the blood.
  • Irritant drugs can be administer by the IV route without risking tissue injury.
  • IV drug administration is expensive, inconvenient and more difficult than administration by other routes.
  • Other disadvantages include the risk of fluid overload, infection, and embolism.  Some drug formulations are completely unsafe for use intravenously.

Intramuscular:

  • Only the capillary wall separates the drug from the blood, so there is not a significant barrier to the drug's absorption.
  • The rate of absorption varies with the drug's solubility and the blood flow at the site of injection.
  • The IM route is uncomfortable and inconvenient for the patient, and if administered improperly, can lead to tissue or nerve damage.

Subcutaneous

Same characteristics as the IM route.

Oral

  • Two barriers to cross: epithelial cells and capillary wall.  To cross the epithelium, drugs have to pass through the cells.
  • Highly variable drug absorption influenced by many factors:  pH, drug solubility and stability, food intake, other drugs, etc.
  • Easy, convenient, and inexpensive.  Safer than parenteral injection, so that oral administration is generally the preferred route.
  • Some drugs would be inactivated by this route
  • Inappropriate route for some patients.
  • May have some GI discomfort, nausea and vomiting.
  • Types of oral meds = tablets, enteric-coated, sustained-release, etc.
  • Topical, Inhalational agents, Suppositories

Carbenicillin

Antibiotic that is chemically similar to ampicillin. Active against gram-negative germs. It is well soluble in water and acid-labile.

Quinolone

Quinolones and fluoroquinolones form a group of  broad-spectrum antibiotics. They are derived from nalidixic acid.

Fluoroquinolone antibiotics are highly potent and considered relatively safe.

MOA : Quinolones act by inhibiting the bacterial  DNA gyrase enzyme. This way they inhibit nucleic acid synthesis and act bacteriocidically.

Drugs  :Nalidixic acid, Ciprofloxacin , Levofloxacin,  Norfloxacin ,Ofloxacin,  Moxifloxacin  , Trovafloxacin

Monoamine oxidase inhibitors (MAOIs) 

e.g. phenelzine, tranylcypromine, moclobemide

- Belong to first generation antidepressants with TCAs
- Most MAOIs irreversibly inhibit the intraneuronal catabolism of norepinephrine and serotonin by MAO-A and MAO-B
- increase brain levels of noradrenaline and 5-HT
- Moclobemide causes selective, reversible inhibition of MAO-A

DRUG INTERACTIONS

Hypertensive crises similar to cheese reaction with OTC cough/cold preparations containing indirect-sympathomimetics
e.g. ephedrine

- Other antidepressants should not be started at least 2 weeks after stopping MAOIs and vice versa due to risk of serotonin syndrome
- Similar interaction with pethidine

ADVERSE DRUG REACTIONS

- Antimuscarinic side effects (e.g. dry mouth, blurred vision, urinary retention)vision, urinary retention)
- Excessive central stimulation causes tremors, excitement and insomnia
- Postural hypotension
- Increased appetite with weight gain

Clavulanic acid is often combined with amoxicillin to treat certain infections caused by bacteria, including infections of the ears, lungs, sinus, skin, and urinary tract. It works by preventing bacterium that release beta-lactamases from destroying amoxicillin.

Diphenoxylate (present in Lomotil)

  • A meperidine congener
  • Not absorbed very well at recommended doses.
  • Very useful in the treatment of diarrhea.

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