Everything about Clindamycin totally explained
| PubChem=29029
| DrugBank=APRD00566
| C=18 | H=33 | Cl=1 | N=2 | O=5 | S=1
|molecular_weight = 424.98 g/mol
|synonyms=7-chloro-lincomycin
7-chloro-7-deoxylincomycin
|bioavailability = 90% (oral)
4–5% (topical)
|metabolism =
Hepatic
|protein_bound = 90%
|elimination_half-life = 2–3 hours
|excretion = Biliary and
renal (around 20%)
|pregnancy_US = B
|pregnancy_AU = A
|legal_AU = S4
|legal_UK = POM
|legal_US = Rx-only
|routes_of_administration = Oral,
topical,
IV,
intravaginal
}}
Clindamycin (
rINN; ) is a
lincosamide antibiotic. It is usually used to treat
infections with
anaerobic bacteria but can also be used to treat some
protozoal diseases, such as
malaria. It is a common
topical treatment for
acne, and can be useful against some
methicillin-resistant Staphylococcus aureus (MRSA) infections.
Clindamycin is marketed alone and in combination with other drugs under various
trade names, including
Dalacin and
Cleocin (manufactured by
Pfizer), in a foam as
Evoclin and
Duac (with
benzoyl peroxide, made by
Stiefel), and a gel form by the name of
Benzaclin, manufactured by
Sanofi Aventis. It is also available as a
generic drug.
Indications
Clindamycin is used primarily to treat infections caused by susceptible
anaerobic bacteria, including infections of the
respiratory tract,
septicemia and
peritonitis. In patients with
hypersensitivity to
penicillins, clindamycin may be used to treat infections caused by susceptible
aerobic bacteria as well. It is also used to treat bone and joint infections, particularly those caused by
Staphylococcus aureus.
Combination therapy in acne
Multiple studies have shown the use of clindamycin in conjunction with benzoyl peroxide, which is available both through prescription or
over-the-counter, to be more effective in the treatment of acne than the use of either product by itself. A
single-blind study comparing this combination to
adapalene, a
retinoid, also found it to work faster and be significantly better tolerated than adapalene, as well as more effective.
Clindamycin and adapalene in combination are also more effective than either drug alone, although adverse effects are more frequent; a single study found with adapalene (application of adapalene 3–5 minutes before clindamycin) to significantly increase the penetration of clindamycin into the skin, which may enhance efficacy.
Malaria
Given with
chloroquine or
quinine, clindamycin is effective and well-tolerated in treating
Plasmodium falciparum malaria; the latter combination is particularly useful for children, and is the treatment of choice for pregnant women who become infected in areas where
resistance to chloroquine is common. Clindamycin shouldn't be used as an antimalarial by itself, although it appears to be very effective as such, because of its slow action. often in combination with a
bactericidal agent such as
vancomycin. The rationale for this approach is a presumed synergy between the bactericidal antibiotic, which causes the death of the bacteria by
breakdown of the cell membrane, and clindamycin, which is a powerful inhibitor of
toxin synthesis. Both
in vitro and
in vivo studies have shown that clindamycin reduces the production of
exotoxins by staphylococci; it may also induce changes in the surface structure of bacteria that make them more sensitive to
immune system attack (
opsonization and
phagocytosis).
It can also be useful in skin and
soft tissue infections caused by
methicillin-resistant Staphylococcus aureus (MRSA); many strains of MRSA are still susceptible to clindamycin.
Clindamycin has been proven to decrease the risk of
premature births in women diagnosed with
bacterial vaginosis during early pregnancy to about a third of the risk of untreated women.
The combination of clindamycin and quinine is the standard treatment for severe
babesiosis. Clindamycin may also be used to treat
toxoplasmosis, and, in combination with
primaquine, is effective in treating mild to moderate
Pneumocystis jirovecii pneumonia.
Susceptible bacteria
It is most effective against infections involving the following types of organisms:
Available forms
Clindamycin preparations for oral administration include capsules (containing clindamycin
hydrochloride) and oral suspensions (containing clindamycin
palmitate hydrochloride).
It is also available for topical administration, in
gel form and in a foam delivery system (both containing clindamycin
phosphate), primarily as a prescription acne treatment.
It is also available in the form of vaginal suppositories, in combination with Clotrimazole IP, as in India, sold as "Clinsup-V" and is manufactured by Olive Health Care. The combination of clindamycin and benzoyl peroxide in a single product is also available, as is (in the United States) a combination of clindamycin and
tretinoin, sold as
Ziana.
Clindamycin is available as a
generic drug, for both systemic (oral and intravenous) and topical use.
Adverse effects
Common
adverse drug reactions (ADRs) associated with clindamycin therapy—found in over 1% of patients—include: diarrhea,
pseudomembranous colitis,
nausea,
vomiting,
abdominal pain or
cramps,
rash, and/or
itch. High
both intravenous and oral doses may cause a metallic taste, and topical application may cause
contact dermatitis.
Pseudomembranous colitis is a potentially-lethal condition commonly associated with clindamycin, but which also occurs with other antibiotics.
Pharmacology
Pharmacokinetics
Approximately 90% of an oral dose of clindamycin is absorbed from the
gastrointestinal tract and it's widely distributed throughout the body, excluding the
central nervous system. Adequate therapeutic concentrations can be achieved in
bone. There is also active uptake into
white blood cells, most importantly
neutrophils.
Clindamycin is extensively
metabolised in the liver, probably by
CYP3A4; some of its metabolites are active, such as
N-dimethyl clindamycin and clindamycin
sulfoxide. The
elimination half-life is 1.5 to 5 hours. Clindamycin is primarily eliminated by hepatic metabolism; after an intravenous dose of clindamycin phosphate, about 4.5% of the dose is excreted in urine as clindamycin and about 0.35% as the phosphate salt. The metabolites are excreted primarily in the urine.
Mechanism of action
Clindamycin has a
bacteriostatic effect. It interferes with bacterial
protein synthesis (in a similar way to
erythromycin,
azithromycin and
chloramphenicol), by binding preferentially to the
50S subunit of the bacterial
ribosome.
The structures of the complexes between several antibiotics (including clindamycin) and a
Deinococcus radiodurans ribosome have been solved by
X-ray crystallography by a team from the
Max Planck Working Groups for Structural Molecular Biology, and published in the journal
Nature.
Interactions
Clindamycin may prolong the effects of
neuromuscular-blocking drugs. Its similarity to the mechanism of action of
macrolides and chloramphenicol means they shouldn't be given simultaneously, as this causes antagonism skin infections, and
toxoplasmosis, for which it's the drug of choice in dogs and cats. Toxoplasmosis rarely causes symptoms in cats, but can do so in very young or
immunocompromised kittens and cats. Toxoplasmosis is contagious to humans, and therefore cat owners, particularly pregnant women, should take precautions to prevent the spread of the disease.
Further Information
Get more info on 'Clindamycin'.
|
External Link Exchanges
Do you know how hard it is to get a link from a large encyclopaedia? Well we're different and will prove it. To get a link from us just add the following HTML to your site on a relevant page:
<a href="http://clindamycin.totallyexplained.com">Clindamycin Totally Explained</a>
Then simply click through this link from your web page. Our crawlers will verify your link, extract the title of your web page and instantly add a link back to it. If you like you can remove the words Totally Explained and embed the link in article text.
As long as your link remains in place, we'll keep our link to you right here. Please play fair - our crawlers are watching. Your site must be closely related to this one's topic. Any kind of spamming, dubious practises or removing the link will result in your link from us being dropped and, potentially, your whole site being banned. |
