Arestin - General Information
A tetracycline analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant staphylococcus infections.
Pharmacology of Arestin
Arestin, the most lipid soluble and most active tetracycline antibiotic, is, like doxycycline, a long-acting tetracycline. Arestin's effects are related to the inhibition of protein synthesis. Although minocycline's broader spectrum of activity, compared to other members of the group, includes activity against Neisseria meningitidis, its use as a prophylaxis is no longer recomended because of side effects (dizziness and vertigo). Current research is examining the possible neuroprotective effects of minocycline against progression of Huntington's Disease, an inherited neurodegenerative disorder. The neuroprotective action of minocycline may include its inhibitory effect on 5-lipoxygenase, an inflammatory enzyme associated with brain aging.
Arestin for patients
Photosensitivity manifested by an exaggerated sunburn reaction has been observed in some individuals taking tetracyclines. Patients apt to be exposed to direct sunlight or ultraviolet light should be advised that this reaction can occur with tetracycline drugs, and treatment should be discontinued at the first evidence of skin erythema. This reaction has been reported rarely with use of minocycline.
Patients who experience central nervous system symptoms should be cautioned about driving vehicles or using hazardous machinery while on minocycline therapy.
Concurrent use of tetracycline may render oral contraceptives less effective.
Because tetracyclines have been shown to depress plasma prothrombin activity, patients who are on anticoagulant therapy may require downward adjustment of their anticoagulant dosage.
Since bacteriostatic drugs may interfere with the bactericidal action of penicillin, it is advisable to avoid giving tetracycline-class drugs in conjunction with penicillin.
Absorption of tetracyclines is impaired by antacids containing aluminum, calcium or magnesium, and iron-containing preparations.
The concurrent use of tetracycline and methoxyflurane has been reported to result in fatal renal toxicity.
Concurrent use of tetracyclines with oral contraceptives may render oral contraceptives less effective.
This drug is contraindicated in persons who have shown hypersensitivity to any of the tetracyclines.
Additional information about Arestin
Arestin Indication: For the treatment of infections caused by susceptible strains of microorganisms, such as Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsial pox and tick fevers caused by Rickettsiae, upper respiratory tract infections caused by Streptococcus pneumoniae and for the treatment of asymptomatic carriers of Neisseria meningitidis.
Mechanism Of Action: Arestin passes directly through the lipid bilayer or passively diffuses through porin channels in the bacterial membrane. Tetracyclines like minocycline bind to the 30S ribosomal subunit, preventing the binding of tRNA to the mRNA-ribosome complex and interfering with protein synthesis.
Drug Interactions: Acitretin Increased risk of intracranial hypertension
Aluminium Formation of non-absorbable complexes
Amoxicillin Possible antagonism of action
Ampicillin Possible antagonism of action
Azlocillin Possible antagonism of action
Aztreonam Possible antagonism of action
Bacampicillin Possible antagonism of action
Carbenicillin Possible antagonism of action
Clavulanate Possible antagonism of action
Cloxacillin Possible antagonism of action
Cyclacillin Possible antagonism of action
Dicloxacillin Possible antagonism of action
Flucloxacillin Possible antagonism of action
Hetacillin Possible antagonism of action
Methicillin Acyl-Serine Possible antagonism of action
Mezlocillin Possible antagonism of action
Nafcillin Possible antagonism of action
Oxacillin Possible antagonism of action
Penicillin G Possible antagonism of action
Penicillin V Possible antagonism of action
Piperacillin Possible antagonism of action
Pivampicillin Possible antagonism of action
Pivmecillinam Possible antagonism of action
Tazobactam Possible antagonism of action
Ticarcillin Possible antagonism of action
Zinc Formation of non-absorbable complexes
Trisalicylate-choline Formation of non-absorbable complexes
Magnesium oxide Formation of non-absorbable complexes
Magnesium Formation of non-absorbable complexes
Salicylate-magnesium Formation of non-absorbable complexes
Iron Formation of non-absorbable complexes
Bismuth Formation of non-absorbable complexes
Calcium Formation of non-absorbable complexes
Attapulgite Formation of non-absorbable complexes
Bismuth Subsalicylate Formation of non-absorbable complexes
Anisindione The tetracycline increases the anticoagulant effect
Acenocoumarol The tetracycline increases the anticoagulant effect
Dicumarol The tetracycline increases the anticoagulant effect
Warfarin The tetracycline increases the anticoagulant effect
Digoxin The tetracycline increases the effect of digoxin in 10% of patients
Insulin The tetracycline increases the risk of hypoglycemia
Methoxyflurane The tetracycline increases the renal toxicity of methoxyflurane
Ethinyl Estradiol This anti-infectious agent could decrease the effect of the oral contraceptive
Mestranol This anti-infectious agent could decrease the effect of the oral contraceptive
Etretinate Increased risk of intracranial hypertension
Isotretinoin This anti-infectious agent could decrease the effect of the oral contraceptive
Food Interactions: Take with food.
Do not take Aluminum or magnesium antacids or supplements while on this medication.
Generic Name: Minocycline
Synonyms: Not Available
Drug Category: Anti-Bacterial Agents; Tetracyclines
Drug Type: Small Molecule; Approved
Other Brand Names containing Minocycline: Alti-Minocycline; Apo-Minocycline; Arestin; Dynacin; Gen-Minocycline; Klinomycin; Minociclina [Inn-Spanish]; Minocin; Minocyclin; Minocycline HCl; Minocyclinum [Inn-Latin]; Minocyn; Minomycin; Novo-Minocycline; Vectrin;
Absorption: Rapidly absorbed from the gastrointestinal tract and absorption is not significantly impaired by ingestion of food or milk. Oral bioavailability is 100%.
Toxicity (Overdose): Minocycline has been observed to cause a dark discoloration of the thyroid in experimental animals (rats, minipigs, dogs and monkeys). In the rat, chronic treatment with minocycline has resulted in goiter accompanied by elevated radioactive iodine uptake and evidence of thyroid tumor production. Minocycline has also been found to produce thyroid hyperplasia in rats and dogs. LD50=2380 mg/kg (rat, oral), LD50=3600 mg/kg (mouse, oral)
Protein Binding: 55% to 76%
Half Life: 11-22 hours
Dosage Forms of Arestin: Capsule Oral
Chemical IUPAC Name: (2Z,4S,4aS,5aR,12aS)-2-(amino-hydroxymethylidene)-4,7-bis(dimethylamino)-10,11,12a-trihydroxy-4a,5,5a,6-tetrahydro-4H-tetracene-1,3,12-trione
Chemical Formula: C23H27N3O7
Minocycline on Wikipedia: http://en.wikipedia.org/wiki/Minocycline
Organisms Affected: Enteric bacteria and other eubacteria