Minocycline- Oral

Minocycline- Oral belongs to the pharmacological class of Tetracycline antibiotics.

Minocycline- Oral has been approved to relieve symptoms and also for the treatment and maintenance of Acne vulgaris, Leprosy, Meningococcal disease, Mycobacterium marinum, Nocardiosis, Plague, Prosthetic joint infection, Rheumatoid arthritis, Sexually transmitted infections, Skin and soft tissue infection, Stenotrophomonas maltophilia infection.

Minocycline is a tetracycline antibiotic that is administered Orally. The drug has a rapid onset of action with maximum concentration (Cmax) achieved immediately after the end of infusion and a time to reach maximum concentration (Tmax) of about 1 hour after the start of the start of the therapy. Minocycline- Oral is distributed throughout the body, including into bone tissue, and has a long elimination half-life of approximately 15-18 hours. The drug is primarily eliminated via hepatic metabolism and biliary excretion. As a lipophilic antibiotic, minocycline- Oral readily penetrates cell membranes, including bacterial cells, where it binds to the 30S ribosomal subunit to inhibit bacterial protein synthesis.

The common side effects involved in using Minocycline- Oral are Diarrhea, Nausea, Vomiting, Abdominal pain, Headache, Dizziness, Rash, discoloration of teeth , nails and gums and Itching.

Minocycline- Oral is available in the form of Tablets.

Minocycline- Oral is approved in Germany, Japan, Malaysia, India, the U.K., the U.S, and China.

Minocycline- Oral belongs to the pharmacological class of Tetracycline antibiotics.

Through coordination with cations like magnesium, tetracyclines enter bacterial cells by using OmpF and OmpC porins. This mechanism allows tetracyclines to enter the periplasm, where they dissociate, enabling the lipophilic tetracycline to diffuse into the bacterial cytoplasm. Once inside, tetracyclines prevent aminoacyl-tRNA from binding to the 30S ribosome, effectively inhibiting protein synthesis. This action has been extensively documented in literature, highlighting the importance of tetracyclines in the treatment of bacterial infections.

Minocycline- Oral has been approved to relieve symptoms and also for the treatment and maintenance of Acne vulgaris, Leprosy, Meningococcal disease, Mycobacterium marinum, Nocardiosis, Plague, Prosthetic joint infection, Rheumatoid arthritis, Sexually transmitted infections, Skin and soft tissue infection, Stenotrophomonas maltophilia infection.

Minocycline- Oral is found to be available in the form of Tablets.

Minocycline- Oral can be used in the following treatment:

• Acne vulgaris
• Leprosy
• Meningococcal disease
• Mycobacterium marinum
• Nocardiosis
• Plague
• Prosthetic joint infection
• Rheumatoid arthritis
• Sexually transmitted infections
• Skin and soft tissue infection
• Stenotrophomonas maltophilia infection

Minocycline- Oral can help to relieve symptoms and also for the treatment and maintenance of Acne vulgaris, Leprosy, Meningococcal disease, Mycobacterium marinum, Nocardiosis, Plague, Prosthetic joint infection, Rheumatoid arthritis, Sexually transmitted infections, Skin and soft tissue infection, Stenotrophomonas maltophilia infection.

Minocycline- Oral is approved for use in the following clinical indications:

• Acne vulgaris
• Leprosy
• Meningococcal disease
• Mycobacterium marinum
• Nocardiosis
• Plague
• Prosthetic joint infection
• Rheumatoid arthritis
• Sexually transmitted infections
• Skin and soft tissue infection
• Stenotrophomonas maltophilia infection

• Acinetobacter baumannii infection, multidrug-resistant:

Adults: 4 mg/kg IV initially (not to exceed 200 mg), followed by 2 mg/kg IV q12h (not to exceed 200 mg per dose).

Duration: Treatment duration may vary depending on the severity and site of the infection.

• Acne vulgaris, inflammatory, moderate to severe:

Immediate-release products: The initial oral dose of this medication is 4 mg/kg (not exceeding 200 mg), followed by 2 mg/kg every 12 hours orally, up to a maximum daily dose of 400 mg.

Solodyn and Minolira (extended-release tablets): The recommended oral dose is 1 mg/kg taken once daily.

Treatment should continue for a period of 12 weeks.

• Leprosy:

Adults: 100 mg PO q12h for 6 months or longer.

• Meningococcal disease, chemoprophylaxis after close contact with a patient with invasive disease:

Adults and children over 8 years of age: 100 mg PO q12h for 5 days.

• Mycobacterium marinum:

Adults: 100 mg PO q12h for at least 3 months.

• Nocardiosis:

Adults: 200 mg IV initially, then 100 mg IV q12h for 6-12 months.

• Plague:

Adults: 200 mg IV initially, then 100 mg IV q12h for 10-14 days.

• Prosthetic joint infection:

Adults: 200 mg IV initially, then 100 mg IV q12h for 6-12 weeks or longer.

• Rheumatoid arthritis:

Adults: 100 mg PO q12h for up to 6 months.

• Sexually transmitted infections:

Adults: 100 mg PO q12h for 7 days.

• Skin and soft tissue infection:

Adults: 4 mg/kg IV initially (not to exceed 200 mg), followed by 2 mg/kg IV q12h (not to exceed 200 mg per dose).

Duration: Treatment duration may vary depending on the severity and site of the infection.

• Stenotrophomonas maltophilia infection, multidrug-resistant:

Adults: 4 mg/kg IV initially (not to exceed 200 mg), followed by 2 mg/kg IV q12h (not to exceed 200 mg per dose).

Duration: Treatment duration may vary depending on the severity and site of the infection.

Tablets: 50mg, 75mg, 100mg, 45mg , 55mg , 65mg , 80mg , 90mg ,105mg , 135mg .

Intravenous

• Dosage Adjustments in Kidney Patients:

The manufacturer's labeling does not include specific dosage adjustments, so caution is advised along with a potential adjustment in dosage and/or time interval between doses. Hemodialysis or peritoneal dialysis are not effective methods for removing tetracyclines in significant amounts.

• Dosage Adjustments in Hepatic Impairment Patients:

No dosage adjustments are needed for hepatic impairment.

• Dosage Adjustments in Pediatric Patients:

Acne Vulgaris

• Safety and efficacy of minocycline are not established in patients below 12 years of age.
• The immediate-release products are initially given at a dose of 4 mg/kg PO, not to exceed 200 mg, followed by a maintenance dose of 2 mg/kg/day PO administered every 12 hours, not to exceed 400 mg/day.
• The extended-release tablets, Solodyn, are given at a dose of 1 mg/kg PO once daily for a period of 12 weeks.
• The dosage for Solodyn is based on the patient's weight
• For Minolira, the dosage is also based on the patient's weight, with a recommended dose of 52.5 mg qDay
• For patients weighing between 45-59 kg, 67.5 mg qDay
• For patients weighing between 60-89 kg, and 105 mg qDay
• For patients weighing between 90-125 kg. For patients weighing
• 126-136 kg, the recommended dose is 135 mg qDay

In the case of C. trachomatis or U. urealyticum

• Infections, 100 mg PO is given every 12 hours for 7 days.

In general, for infections,

• The dosing for Minocycline is not recommended for children below 8 years of age unless

• Other antibiotics are not an option. For children 8 years and above, the initial dose is 4 mg/kg PO/IV, not to exceed 200 mg, followed by a maintenance dose of 2 mg/kg PO/IV every 12 hours, not to exceed the adult dose. The recommended dose is not to exceed 100 mg PO/IV every 12 hours for 5-10 days.

There are no specific dietary restrictions related to the use of Minocycline- Oral. However, like with most antibiotics, it is generally recommended to take Minocycline- Oral with a full glass of water and to avoid taking it with milk or other dairy products as they may decrease the absorption of the medication. Additionally, taking Minocycline- Oral with food can help minimize the risk of gastrointestinal upset.

Minocycline- Oral may be contraindicated under the following conditions:

• Patients who have a known hypersensitivity to any component of Minocycline- Oral or to other drugs in the same class.

The physician should closely monitor the patients and keep pharmacovigilance as follows:

Tooth Discoloration and Enamel Hypoplasia

• Use of Tetracycline class drugs during the last half of pregnancy, infancy, and childhood to the age of 8 years may cause permanent discoloration of the teeth and enamel hypoplasia.

Pseudomembranous Colitis

• Antibacterial agents, including Minocycline- Oral tablets, may cause C. difficile-associated diarrhea (CDAD), ranging in severity from mild to fatal colitis.
• CDAD must be considered in all patients who present with diarrhea following antibiotic use.

Photosensitivity

• Photosensitivity manifested by an exaggerated sunburn reaction may occur in some individuals taking tetracyclines.
• Patients exposed to direct sunlight or ultraviolet light should be advised, and treatment should be discontinued at the first evidence of skin erythema.

Superinfection

• Use of Minocycline- Oral may result in overgrowth of non-susceptible organisms, including fungi.
• Appropriate therapy should be instituted if superinfection occurs.

Benign Intracranial Hypertension

• Bulging fontanels in the infants and the benign intracranial hypertension in adults had been reported in individuals receiving tetracyclines.
• These conditions disappeared when the drug had been discontinued.

Growth and Development

• All tetracyclines forms a stable calcium complex in any bone-forming tissue, and toxic effects on the developing fetus have been observed in animals treated early in pregnancy.
• Patients using tetracyclines during pregnancy should be aware of potential hazards to the fetus.

Antianabolic Action and Laboratory Monitoring

• The antianabolic action of the tetracyclines might cause an increase in BUN.
• The organ systems, including hematopoietic, renal, and hepatic, should undergo periodic laboratory evaluation during long-term therapy.

Malaria and Development of Drug Resistant Bacteria

• Minocycline- Oral provides significant, but not complete, suppression of the asexual blood stages of Plasmodium strains that cause malaria.
  
• Prescribing Minocycline- Oral without a proven or strongly suspected bacterial infection or prophylactic indication increases the risk of developing drug-resistant bacteria.
  

Syphilis Testing

• When syphilis is suspected in venereal disease cases, dark-field examinations should be conducted before treatment initiation, and blood serology should be repeated monthly for at least 4 months

Incision and Drainage

• Antibiotic therapy should be performed in conjunction with incision and drainage or other surgical procedures when indicated.

There is no specific alcohol warning associated with the use of Minocycline- Oral. However, it is generally recommended to avoid excessive alcohol consumption while taking antibiotics as it can interfere with the effectiveness of the medication and may also increase the risk of certain side effects such as nausea, vomiting, and dizziness.

Tetracyclines are eliminated in human breast milk. Due to the risk of significant adverse effects in breastfed infants, a decision must be made about whether to stop nursing or cease taking the medication, taking into account the importance of the drug to the mother.

Pregnancy Category D:

Regardless of drug exposure, all pregnancies carry a background risk of birth defects, loss, or other adverse outcomes. There is currently a lack of adequate and well-controlled studies on the usage of minocycline in pregnant women. Minocycline, similar to other antibiotics within the tetracycline class, has the ability to cross the placenta and potentially cause harm to a developing fetus when administered to a pregnant woman. There have been some rare spontaneous reports of congenital anomalies, including limb reduction, in post-marketing experiences. The information on these reports is limited, hence it is not possible to establish a conclusive causal relationship. In the event that minocycline is administered during pregnancy or if the patient becomes pregnant while taking this medication, it is important to make the patient aware of the potential risk to the developing fetus.

Minocycline oral should be taken with caution or avoided with dairy products, calcium supplements, iron supplements, magnesium supplements, zinc supplements, and antacids containing aluminum, magnesium, or calcium, as these can bind to minocycline and reduce its absorption from the gastrointestinal tract. This can lead to reduced effectiveness of the medication. To avoid this interaction, minocycline should be taken at least 2 hours before or after these products.

The adverse reactions related to Minocycline- Oral can be categorized as follows:

Common

• Nausea
• Vomiting
• Dizziness
• Diarrhea
• Headache
• Skin rash
• Pruritus (itching)
• Abdominal pain
• Hypertension (high blood pressure)
• Phlebitis (inflammation of a vein)

Less Common

• Anorexia (loss of appetite)
• Photosensitivity (increased sensitivity to sunlight)
• Asthenia (weakness or lack of energy)
• Dyspnea (shortness of breath)
• Chest pain
• Tachycardia (rapid heart rate)
• Arthralgia (joint pain)
• Myalgia (muscle pain)
• Hyperpigmentation (excess pigmentation of the skin)
• Urinary tract infection

Rare

• Hypersensitivity reactions (e.g. anaphylaxis, angioedema)
• Hepatotoxicity (liver damage)
• Renal failure
• Blood dyscrasias (abnormalities in blood cell counts)
• Intracranial hypertension (increased pressure inside the skull)

The clinically relevant drug interactions of Minocycline- Oral are briefly summarized here:

• Anticoagulant Drugs:

Tetracyclines have been found to reduce plasma prothrombin activity. As a result, patients who are on anticoagulant therapy may require a lower anticoagulant dose.

• Penicillin:

Bacteriostatic drugs might interfere with the bactericidal action of penicillin. Therefore, it is recommended to avoid administering tetracyclines along with penicillin.

• Antacids and Iron Preparations:

The absorption of tetracyclines is hindered by antacids that contain aluminum, calcium, or magnesium, bismuth subsalicylate, and iron-containing preparations.

• Oral Contraceptives:

Concurrent use of tetracycline may reduce the effectiveness of oral contraceptives.

• Barbiturates and Anti-Epileptics:

The half-life of Minocycline- Oral is reduced by barbiturates, carbamazepine, and phenytoin.

• Penthrane:

The simultaneous use of tetracycline and Penthrane® (methoxyflurane) has been linked to fatal renal toxicity.

The following are the side effects involving Minocycline- Oral:

• Nausea and vomiting
• Dizziness
• Headache
• Rash
• Diarrhea
• Discoloration of skin, teeth, nails, or gums
• Yeast infections

Pregnancy:

Pregnancy Category D:

Regardless of drug exposure, all pregnancies carry a background risk of birth defects, loss, or other adverse outcomes. There is currently a lack of adequate and well-controlled studies on the usage of minocycline in pregnant women. Minocycline, similar to other antibiotics within the tetracycline class, has the ability to cross the placenta and potentially cause harm to a developing fetus when administered to a pregnant woman. There have been some rare spontaneous reports of congenital anomalies, including limb reduction, in post-marketing experiences. The information on these reports is limited, hence it is not possible to establish a conclusive causal relationship. In the event that minocycline is administered during pregnancy or if the patient becomes pregnant while taking this medication, it is important to make the patient aware of the potential risk to the developing fetus.

Nursing Mothers

Tetracyclines are eliminated in human breast milk. Due to the risk of significant adverse effects in breastfed infants, a decision must be made about whether to stop nursing or cease taking the medication, taking into account the importance of the drug to the mother.

Pediatric Use

This medication should not be administered to patients who are under the age of eight.

Geriatric Use

Clinical trials involving intravenous minocycline did not involve enough participants aged 65 years and older to ascertain whether they react differently than younger individuals. As a general rule, when it comes to elderly patients, caution should be exercised in the selection of the dosage. This usually means starting at the lower end of the dosage spectrum, given the more common occurrence of reduced hepatic, renal, or cardiac function, as well as coexisting illnesses or concomitant drug treatment.

Physicians should be knowledgeable as well as vigilant about the treatment and identification of overdosage of Minocycline- Oral .

The most frequently observed adverse events in cases of minocycline overdose are dizziness, nausea, and vomiting. There is currently no known specific antidote for minocycline overdose.

If an overdose is suspected, it is recommended to discontinue the medication and manage the symptoms through appropriate supportive measures. It should be noted that minocycline is not significantly eliminated through hemodialysis or peritoneal dialysis.

Pharmacodynamics

Microbial Activity

• Active against Rickettsiae (Rocky Mountain spotted fever, typhus fever and the typhus group, Q fever, rickettsial pox, tick fevers), Mycoplasma pneumoniae (PPLO, Eaton agent), agents of psittacosis and ornithosis, agents of lymphogranulomavenereum and granuloma inguinale, the spirochetal agent of relapsing fever (Borrelia recurrentis), Haemophilus ducreyi (chancroid), Yersinia pestis, Pasteurella pestis and Pasteurella tularensis, Bartonella bacilliformis, Bacteroides species, Vibrio comma and Vibrio fetus, and Brucella species (in conjunction with streptomycin).

Pharmacokinetics

Characteristics of oral minocycline absorption:

● 100mg of oral minocycline results in a Cmax of 1.6mg/L, Tmax of 1.9h, and AUC of 31.6mg/L*h.

● 200mg of oral minocycline results in a Cmax of 3.1mg/L, Tmax of 2.5h, and AUC of 48.3mg/L*h.

Volume of distribution:

The volume of distribution of minocycline ranges from 67.5-115L.

Protein binding:

Minocycline is 76% protein bound in serum.

Metabolism:

Minocycline undergoes metabolism primarily to 9-hydroxyminocycline, as well as to 2 different N-demethylated metabolites.

Route of elimination:

Minocycline is predominantly eliminated via the biliary route, with 4.5-9% of an intravenous dose and 10-19.5% of an oral dose recovered in urine, and 20-34% of an oral dose recovered in feces.

• https://www.mayoclinic.org/drugs-supplements/minocycline-intravenous-route/description/drg-20122784
• https://reference.medscape.com/drug/dynacin-minocin-minocycline-342549
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• https://go.drugbank.com/drugs/DB01017
• https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050649023lbl.pdf
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