Quintos Kevin D.

Bsn 131

Pharmacology Assignment

Roxithromycin

Roxithromycin is a semi-synthetic macrolide antibiotic. It is used to treat respiratory

tract, urinary and soft tissue infections. Roxithromycin is derived from erythromycin,
containing the same 14-membered lactone ring. However, an N-oxime side chain is
attached to the lactone ring. It is also currently undergoing clinical trials for the treatment
of male-pattern hair loss.[1]
Roxithromycin is available under several brandnames, for example, Roxl-150, Roxo,
Surlid, Rulide, Biaxsig, Roxar, Roximycin, Roxomycin, Tirabicin and Coroxin.
Roxithromycin is not available in the United States. Roxithromycin has also been tested
to possess antimalarial activity.

History
German pharmaceutical company Hoechst Uclaf brought out roxithromycin in 1987.

Available forms
Roxithromycin is commonly available as tablets or oral suspension.

Mechanism of action
Roxithromycin prevents bacteria from growing, by interfering with their protein
synthesis. Roxithromycin binds to the subunit 50S of the bacterial ribosome, and thus
inhibits the translocation of peptides. Roxithromycin has similar antimicrobial spectrum
as erythromycin, but is more effective against certain gram-negative bacteria,
particularly Legionella pneumophila.

Pharmacokinetics
When taken before a meal, roxithromycin is very rapidly absorbed, and diffused into
most tissues and phagocytes. Due to the high concentration in phagocytes,
roxithromycin is actively transported to the site of infection. During active phagocytosis,
large concentrations of roxithromycin are released.

Metabolism
Only a small portion of roxithromycin is metabolised. Most of roxithromycin is secreted
unchanged into the bile and some in expired air. Under 10% is excreted into the urine.
Roxithromycin's half-life is 12 hours.

Side effects
Most common side effects are gastrointestinal; diarrhoea, nausea, abdominal pain and
vomiting. Less common side effects include central or peripheral nervous system events
such as headaches, dizziness, vertigo, and also the rarely seen rashes, abnormal liver
function values and alteration in senses of smell and taste.
Quintos Kevin D. Bsn 131

Drug interactions
Roxithromycin has fewer interactions than erythromycin as it has a lower affinity for
cytochrome P450.
Roxithromycin does not interact with hormonal contraceptives, prednisolone,
carbamazepine, ranitidine or antacids.

When roxithromycin is administered with theophylline, some studies have shown an

increase in the plasma concentration of theophylline. A change in dosage is usually not
required but patients with high levels of theophylline at the start of the treatment should
have their plasma levels monitored.
Roxithromycin appears to interact with warfarin. This is shown by an increase in
prothrombin time (international normalised ratio [INR]) in patients taking roxithromycin
and warfarin concurrently. As a consequence, severe bleeding episodes have occurred.

Drug Dosage & efficacy per weight and age

Adults: 300mg per day.

Mode of Administration Oral route; Swallow the Pharmacokinetic data

tablet with a glass of water.

Bioavailability ?

Therapeutic considerations
Roxithromycin
Pregnancy cat. ? (USA)
B1 (Aus)

Chemical data

Formula C41H76N2O15

Systematic (IUPAC) name Mol. mass 837.047 g/mol

From Wikipedia.org

ROXITHROMYCIN

Article
Quintos Kevin D. Bsn 131

Effects of oral antibiotic roxithromycin on quality of life in acne patients

Miwa KOBAYASHI, Kenji KABASHIMA, Motonobu NAKAMURA, Yoshiki TOKURA
Department of Dermatology, University of Occupational and Environmental
Health Japan, Kitakyushu, Japan
Correspondence: Miwa Kobayashi, M.D., PhD., Department of Dermatology,
University of Occupational and Environmental Health, 1-1 Iseigaoka, Yahatanishi-
ku, Kitakyushu 807-8555, Japan. Email: miw-koba@med.uoeh-u.ac.jp

ABSTRACT
Macrolides are effective for inflammatory acne, but there are not many studies on
roxithromycin. In this study, patients with acne were surveyed for improvement of their
quality of life after treatment with roxithromycin. Patients were orally given roxithromycin
300 mg daily for 2–4 weeks. At the time of pre- and post-treatment, the dermatologists
graded the severity of acne symptoms, and the patients answered questionnaires. In
123 half faces of 76 patients, 80 half faces were improved, 42 half faces were not
changed, and one half face was deteriorated. The score of "symptom and feeling" and
"leisure" in DLQI-J and "emotions" and "symptoms" in Skindex-29-J were significantly
decreased after roxithromycin treatment. Roxithromycin has a therapeutic effect on
inflammatory acne and leads to improvement of quality of life in the patients.

Received: 28 July 2008; accepted: 23 November 2008

- I am one of those teen agers who suffer from acne. It has always been my
problem since I was 14. It is really good to know that there is a new study about
medications aside from those that I apply on my face (like creams and facila
wash) that can help me and other teens that suffer from the same problem. I
hope that there will be new improvements about this drug.With this teen agers
like me can not only improve our physical appearance but also it can boost our
morale and confidence therefore improving our quality of life as mentioned in the
article.