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Clarithromycin

Trade name Biaxin

Routes of administration, oral, intravenous.

Bioavailability 50%.

Protein binding is low.

Hepatic metabolism.

Biological half-life 3–4 hours.

An antibiotic used to treat various bacterial infections including.: strep throat, pneumonia, skin infections, H. pylori infection, and Lyme disease, among others.

Can be taken by mouth as a pill or liquid.

Common side effects include nausea, vomiting, headaches, and diarrhea.

It may cause harm if taken during pregnancy.

Works by stopping the making of protein by some bacteria.

Made from erythromycin.

Primarily used to treat a number of bacterial infections including: pneumonia, Helicobacter pylori and as an alternative to penicillin in strep throat.

Other infections include: cat scratch disease infections due to bartonella, cryptosporidiosis, as a second line agent in Lyme disease and toxoplasmosis.

Ued to prevent bacterial endocarditis in those who cannot take penicillin.

Efficacious against upper and lower respiratory tract infections, skin and soft tissue infections and helicobacter pylori infections associated with duodenal ulcers.

Spectrum of bacterial susceptibility:

Aerobic Gram-positive bacteria

Staphylococcus aureus

Streptococcus pneumoniae

Streptococcus pyogenes

Aerobic Gram-negative bacteria

Haemophilus parainfluenzae

Haemophilus influenzae

Moraxella catarrhalis

Helicobacter pylori

Mycobacteria

Mycobacterium avium complex

Chlamydia pneumoniae

Mycoplasma pneumoniae

Clarithromycin should not be used with a history of cholestatic jaundice and/or liver dysfunction associated with prior clarithromycin use.

Should not be used with hypokalaemia.

Use of clarithromycin with pimozide, astemizole, terfenadine, ergotamine, ticagrelor, ranolazine or dihydroergotamine is not recommended.

It should not be used with colchicine, in people with kidney or liver impairment, with cholesterol medications such as lovastatin or simvastatin, hypersensitivity to clarithromycin or any component of the product, erythromycin, or any macrolide antibiotics, with QT prolongation or ventricular cardiac arrhythmias, including torsade de pointes.

The most common side effects are gastrointestinal: diarrhea (3%), nausea (3%), abdominal pain (3%), and vomiting (6%).

May be associated with headaches, insomnia, and abnormal liver function tests.

Allergic reactions include rashes and anaphylaxis.

Rarely associated with extreme irritability, hallucinations, dizziness, motion sickness, and alteration in senses of smell and taste, including a metallic taste, dry mouth, panic attacks, and nightmares.

Can lead to a prolonged QT interval, and can increase risk for life-threatening arrhythmias.

Use of short-term treatment is correlated with an increased incidence of deaths classified as sudden cardiac deaths in stable coronary heart disease patients not using statins.

Known to cause jaundice, cirrhosis, and kidney problems, including renal failure.

Common adverse effects in the central nervous system include dizziness, headaches.

Rarely, it can cause ototoxicity, delirium and mania.

Associated with increase risk of oral candidiasis.

Should not be used in pregnant women except in situations where no alternative therapy is appropriate.

Can cause potential hazard to the fetus hence should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Not known whether it is excreted in human milk.

Inhibits a liver enzyme, CYP3A4, involved in the metabolism of many other commonly prescribed drugs, and concomitant administration with other medications that are metabolized by CYP3A4 may lead to unexpected increases or decreases in drug levels.

Has dangerous interaction with colchicine as the result of inhibition of CYP3A4 metabolism and P-glycoprotein transport.

Combining these two drugs may lead to fatal colchicine toxicity, particularly in patients with renal insufficiency.

Taking clarithromycin concurrently with certain statins increases the risk of side effects, such as muscle aches and rhabdomyolysis.

Concurrent therapy with calcium channel blocker may increase risk of low blood pressure, kidney failure, and death, compared to treating calcium channel blockers with azithromycin, a drug similar to clarithromycin but without CYP3A4 inhibition.

Administration of clarithromycin in combination with verapamil have been observed to cause low blood pressure, low heart rate, and lactic acidosis.

May double the level of carbamazepine in the body by reducing its clearance, which may lead to toxic symptoms, such as double vision, loss of body movement, nausea, as well as hyponatremia.

May lead to decreased zidovudine concentrations.

Inhibits bacteria by acting as a protein synthesis inhibitor as it binds to 23S rRNA, a component of the 50S subunit of the bacterial ribosome, thus inhibiting the translation of peptides.

Unlike erythromycin, it is acid-stable and can be taken orally without having to be protected from gastric acids.

It is readily absorbed, and diffuses into most tissues and phagocytes.

Due to the high concentration in phagocytes, it is actively transported to the site of infection.

During active phagocytosis, large concentrations are released; its concentration in the tissues can be over 10 times higher than in plasma.

Highest concentrations are found in liver, lung tissue, and stool.

Has a fairly rapid first-pass metabolism in the liver.

20%-40% of the drug and 10-15% of its active metabolite are excreted in urine.

Bioavailability at 50%.

Its elimination half-life is about 3 to 4 hours with 250 mg administered every 12 h, but increased to 5 to 7 h with 500 mg administered every 8 to 12 h.

The steady-state concentration of this metabolite is generally attained within 3 to 4 days.

Available as immediate release tablets, extended release tablets, and granules for oral suspension.

Used for treatment of respiratory infections, community acquired pneumonia, and is commonly prescribed in combination with amoxicillin for metronidazole plus proton pump inhibitors as a first-line standard treatment of Helicobacter pylori eradication.

May be associated with neuropsychiatric events in patients with or without comorbitirs such as renal disease, hypertension, and obstructive airway disease.

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