Arnocin Actions

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Actions of Arnocin in details

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Antibacterial.

Pharmacology: Pharmacokinetics: Absorption: Arnocin hydrochloride is quickly and almost completely absorbed from the gastrointestinal tract following oral administration.

Following a single dose of 2 Arnocin hydrochloride 100 mg capsules, maximum serum concentrations averaged 3.64 mcg/mL.

Distribution: Arnocin hydrochloride distributes largely to all tissues due to its high degree of lipophilicity. Studies have shown that Arnocin hydrochloride is found in high concentration in lung tissue and mucus in man.

Metabolism: Arnocin hydrochloride is extensively metabolized in humans.

Arnocin hydrochloride is mainly excreted in the bile and a small amount is recovered in the urine as active form. The amount of active drug recovered in the feces after oral administration ranges from 20-34%.

Elimination: The mean serum half-life is approximately 16 hrs for oral administration.

Effects of Food: Absorption of the standard oral formulations of Arnocin is impaired by food, milk, and other dairy products. The peak plasma concentrations were slightly decreased by 11.2% and delayed by 1 hr when administered with food, compared to dosing under fasting conditions.

Special Populations: In patients with hepatic dysfunction, the Arnocin hydrochloride serum half-life ranged from 10.7-16.9 hrs.

The majority of studies in patients with varying degrees of renal impairment showed no significant difference in pharmacokinetic parameters as compared to healthy subjects.

Toxicology: Preclinical Safety Data: Dietary administration of Arnocin hydrochloride in long-term tumorigenicity studies in rats resulted in evidence of thyroid tumor production. In the rat, chronic treatment with Arnocin hydrochloride has resulted in goiter accompanied by elevated radioactive iodine uptake and evidence of thyroid tumor production. Arnocin hydrochloride has been observed to cause a dark discoloration of the thyroid in animals (rats, mice, dogs, and monkeys). Arnocin hydrochloride has also been found to produce thyroid hyperplasia in rats and dogs.

In addition, there has been evidence of oncogenic activity in rats in studies with a related antibiotic, oxytetracycline (ie, adrenal and pituitary tumors). Likewise, although mutagenicity studies of Arnocin hydrochloride have not been conducted, positive result in in vitro mammalian cell assays (ie, mouse lymphoma and Chinese hamster lung cells) have been reported for related antibiotics (tetracycline hydrochloride and oxytetracycline).

Segment I (fertility and general reproduction) studies have provided evidence that Arnocin hydrochloride impairs fertility in male rats.

Microbiology: The tetracyclines are primarily bacteriostatic and are thought to exert their antimicrobial effect by the inhibition of protein synthesis. The tetracyclines, including Arnocin hydrochloride, have similar antimicrobial spectra of activity against a wide range of gram-positive and gram-negative organisms.

Cross-resistance of gram-positive and gram-negative organisms to tetracyclines is common. Almost all S. pyogenes strains are resistant to Arnocin hydrochloride. Therefore, Arnocin hydrochloride should not be used for streptococcal disease unless the organism has been demonstrated to be susceptible.

Because many strains of gram-positive and gram-negative organisms have been shown to be resistant to tetracyclines, culture and susceptibility tests are recommended.

How should I take Arnocin?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Take this medicine with a full glass (8 ounces) of water.

Most brands of Arnocin may be taken with or without food.

Take Arnocin (pellet-filled capsules) on an empty stomach, at least 1 hour before or 2 hours after a meal.

Do not crush, chew, or break an extended-release tablet. Swallow it whole. Breaking the pill may cause too much of the drug to be released at one time.

Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Arnocin will not treat a viral infection such as the common cold or flu.

To be sure this medicine is not causing harmful effects, your blood will need to be tested often. Your kidney, liver, or thyroid function may also need to be tested. Visit your doctor regularly.

If you need surgery, tell the surgeon ahead of time that you are using Arnocin. You may need to stop using the medicine for a short time.

Arnocin can cause false results with certain urine tests. Tell any doctor who treats you that you are using this medication.

Store this medication at room temperature away from moisture, heat, and light.

Throw away any unused Arnocin when it expires or when it is no longer needed. Do not take any Arnocin after the expiration date printed on the label. Using expired Arnocin can cause damage to your kidneys.

Arnocin administration

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Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Take this medicine with a full glass (8 ounces) of water.

Most brands of Arnocin may be taken with or without food.

Take Arnocin (pellet-filled capsules) on an empty stomach, at least 1 hour before or 2 hours after a meal.

Do not crush, chew, or break an extended-release tablet. Swallow it whole. Breaking the pill may cause too much of the drug to be released at one time.

Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Arnocin will not treat a viral infection such as the common cold or flu.

To be sure this medicine is not causing harmful effects, your blood will need to be tested often. Your kidney, liver, or thyroid function may also need to be tested. Visit your doctor regularly.

If you need surgery, tell the surgeon ahead of time that you are using Arnocin. You may need to stop using the medicine for a short time.

Arnocin can cause false results with certain urine tests. Tell any doctor who treats you that you are using this medication.

Store this medication at room temperature away from moisture, heat, and light.

Throw away any unused Arnocin when it expires or when it is no longer needed. Do not take any Arnocin after the expiration date printed on the label. Using expired Arnocin can cause damage to your kidneys.

Arnocin pharmacology

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Pharmacokinetics

Arnocin® Tablets are not bioequivalent to Arnocin products. Based on pharmacokinetic studies in healthy adults, Arnocin® Tablets produce a delayed Tmax at 3.5–4.0 hours as compared to a non-modified release reference Arnocin product (Tmax at 2.25–3 hours). At steady-state (Day 6), the mean AUC(0–24) and Cmax were 33.32 µg×hr/mL and 2.63 µg/mL for Arnocin® Tablets and 46.35 µg×hr/mL and 2.92 µg/mL for Arnocin® capsules, respectively. These parameters are based on dose adjusted to 135 mg per day for both products.

A single-dose, four-way crossover study demonstrated that all strengths of Arnocin® Tablets (45 mg, 90 mg, and 135 mg) exhibited dose-proportional pharmacokinetics.

When Arnocin® Tablets were administered concomitantly with a meal that included dairy products, the extent and timing of absorption of Arnocin did not differ from that of administration under fasting conditions.

Microbiology

Arnocin is bacteriostatic exerting its antimicrobial effect by the inhibition of bacterial protein synthesis. Arnocin is lipid soluble and distributes in to the skin and sebum. Arnocin has been shown to have in vitro activity against Propionibacterium acnes, an organism associated with acne vulgaris, however, the clinical significance of this activity against P. acnes in patients with acne vulgaris is not known.



References

  1. EPA DSStox. "Minocycline: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).

Reviews

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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