Actisite

Name: Actisite

Before Using Actisite

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Pediatric

Studies on this medicine have been done only in adult patients, and there is no specific information comparing use of this medicine in children with use in other age groups.

Geriatric

Many medicines have not been studied specifically in older people. Therefore, it may not be known whether they work exactly the same way they do in younger adults or if they cause different side effects or problems in older people. There is no specific information comparing use of this medicine in the elderly with use in other age groups.

Interactions with Medicines

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. Tell your healthcare professional if you are taking any other prescription or nonprescription (over-the-counter [OTC]) medicine.

Interactions with Food/Tobacco/Alcohol

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. Discuss with your healthcare professional the use of your medicine with food, alcohol, or tobacco.

Pharmacology

Mechanism of Action

Inhibits bacterial protein synthesis by binding with 30S and possibly 50S ribosomal subunit(s)

Absorption

Absorption: 75% (PO)

Peak plasma time: 2-4 hr (PO)

Distribution

Small amount appears in bile; relative diffusion from blood into CSF: good only with inflammation (exceeds usual MICs) CSF: blood level ratio: inflamed meninges: 25%

Protein bound: 65%

Elimination

Half-life: 8-11 hr (normal renal function); 57-108 hr (end-stage renal disease)

Excretion: Urine (60% as unchanged drug); feces (as active form)

For Healthcare Professionals

Applies to tetracycline: compounding powder, oral capsule, oral suspension, oral tablet

Gastrointestinal

Gastrointestinal side effects have included anogenital lesions with monilial overgrowth, anorexia, black hairy tongue, dysphagia, enamel hypoplasia, enterocolitis, epigastric distress, diarrhea, glossitis, nausea, permanent tooth discoloration, and vomiting. Rarely, esophageal ulceration has been reported with oral tablets and capsules.[Ref]

There have been several cases of esophageal ulcers associated with oral tetracycline therapy. In each case, the patient had taken the medication just before bedtime with only small amounts of liquid and reported severe retrosternal pain and painful swallowing shortly thereafter. The ulcers resolved spontaneously after discontinuation of tetracycline therapy. To minimize esophageal irritation, patients should be advised to avoid taking tetracycline just before retiring and to take the medication with plenty of water.

Oral ulcers have also occurred in a patient who gargled with a tetracycline solution made by emptying the contents of a 250 mg capsule into water.[Ref]

Renal

Renal side effects generally occurred in patients with preexisting renal disease and have been the result of accumulation of tetracycline (the active ingredient contained in Actisite) Increases in BUN commonly occur because of tetracycline's anti-anabolic effect but do not necessarily indicate renal dysfunction.

Fanconi's syndrome is characterized by renal glycosuria, phosphaturia, aminoaciduria, and acidosis with or without proteinuria and rickets. It is associated with the ingestion of outdated or degraded tetracycline. Additionally, previous formulations of tetracycline contained citric acid which may contribute to metabolic acidosis; however, current formulations of the drug do not. Patients generally require hospitalization with intravenous medication to correct the accompanying metabolic abnormalities. Most cases resolve over time after discontinuation of tetracycline without permanent sequelae. Patients should be instructed to discard any unused portions of tetracycline at the end of therapy and to never use tetracycline remaining from a previous prescription.[Ref]

Renal side effects have included increased BUN and Fanconi's syndrome. In patients with preexisting renal impairment, tetracycline may cause azotemia, hyperphosphatemia, and acidosis. Patients with dehydration are particularly vulnerable.[Ref]

Dermatologic

Dermatologic side effects have included exfoliative dermatitis, maculopapular and erythematous rashes, nail discoloration, onycholysis, and photosensitivity.[Ref]

Musculoskeletal

Musculoskeletal side effects have included adult tooth discoloration, enamel hypoplasia, and a decrease in linear skeletal growth rate. Tetracycline (the active ingredient contained in Actisite) should not be administered to pregnant women or children less than 12 years of age.[Ref]

Tetracycline deposits into calcium-rich developing osseous tissue thereby causing the discoloration of permanent teeth, decreased rate of enamel growth, and a decrease in linear skeletal growth rate.[Ref]

Nervous system

There have been several cases of benign intracranial hypertension (pseudotumor cerebri) associated with tetracycline (the active ingredient contained in Actisite) therapy. In most cases, the patient was female and was prescribed tetracycline to treat acne. Symptoms commonly occurring in these cases consisted of severe headaches, nausea, and blurred vision. Physical examination revealed papilledema in all cases, and several had significantly increased pressure on lumbar puncture. All patients recovered over time after discontinuation of tetracycline therapy. The mechanism for development of increased intracranial pressure is unknown.[Ref]

Nervous system side effects have included benign intracranial hypertension (pseudotumor cerebri) in adults and bulging fontanels in infants.[Ref]

Hematologic

Hematologic side effects have included hemolytic anemia, thrombocytopenia, thrombocytopenic purpura, neutropenia, and eosinophilia.[Ref]

At least two cases of tetracycline-induced hemolytic anemia have been reported. In both cases, the anemia resolved over time after discontinuation of the medication and reoccurred 1 to 2 years later following another course of tetracycline therapy. The mechanism for development of hemolytic anemia is unknown.[Ref]

Hypersensitivity

Hypersensitivity side effects have included urticaria, angioneurotic edema, anaphylaxis, anaphylactoid purpura, exacerbation of systemic lupus erythematosus, hypersensitivity myocarditis, and serum sickness-like reactions (fever, rash, arthralgia).[Ref]

Hepatic

Hepatic side effects have included increased liver enzyme levels, hepatotoxicity, liver failure, and bile duct paucity with prolonged cholestasis. These may be dose-related.[Ref]

Other

Other side effects have included superinfection due to overgrowth of resistant organisms. The long-term use of tetracyclines has been associated with microscopic brown-black discoloration of the thyroid gland; however, abnormal thyroid function has not been reported.[Ref]

Metabolic

Metabolic side effects have included azotemia, hyperphosphatemia, and metabolic acidosis. Increases in serum BUN levels may occur as a result of the anti-anabolic action of tetracycline (the active ingredient contained in Actisite) and not necessarily indicate renal disease.[Ref]

These metabolic side effects have occurred more commonly in the presence of preexisting renal disease, and occur as a result of the accumulation of tetracycline.[Ref]

Some side effects of Actisite may not be reported. Always consult your doctor or healthcare specialist for medical advice. You may also report side effects to the FDA.

Usual Adult Dose for Lyme Disease - Carditis

500 mg orally every 6 hours for 14 to 30 days, depending on the nature and severity of the infection

Usual Adult Dose for Pneumonia

500 mg orally every 6 hours for 10 to 21 days, depending on the nature and severity of the infection

Usual Adult Dose for Psittacosis

500 mg orally 4 times a day; initial treatment with IV doxycycline may be necessary for seriously ill patients
Duration: Treatment should continue at least 10 to 14 days after fever subsides to prevent relapse

Usual Adult Dose for Syphilis - Latent

500 mg orally every 6 hours for 28 days; alternatively, 30 to 40 g in divided doses over a period of 10 to 15 days has been recommended

Tetracycline should be used only if penicillins are contraindicated.

Usual Adult Dose for Tertiary Syphilis

500 mg orally every 6 hours for 28 days

Tetracycline should be used only if penicillins are contraindicated.

Usual Pediatric Dose for Bacterial Infection

Above 8 years of age: 25 to 50 mg/kg orally per day divided in 4 equal doses

Other Comments

Therapy should be continued for at least 1 to 2 days after symptoms and fever have subsided.

In the treatment of streptococcal infections, a therapeutic dose of tetracycline should be given for at least 10 days.

Administration of tetracycline with food, particularly dairy products, significantly reduces absorption. Tetracycline should be administered 1 hour before or 2 hours after meals. Taking the medication with a full glass of water in an upright position will help prevent esophageal ulceration and gastrointestinal irritation.

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