DRUGS & SUPPLEMENTS

Threolone

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Threolone uses

Threolone consists of Chloramphenicol, Prednisolone.

Chloramphenicol:


An antibiotic first isolated from cultures of Streptomyces venequelae in 1947 but now produced synthetically. It has a relatively simple structure and was the first broad-spectrum antibiotic to be discovered. It acts by interfering with bacterial protein synthesis and is mainly bacteriostatic. (From Martindale, The Extra Pharmacopoeia, 29th ed, p106)

Indication: Used in treatment of cholera, as it destroys the vibrios and decreases the diarrhea. It is effective against tetracycline-resistant vibrios. It is also used in eye drops or ointment to treat bacterial conjunctivitis.

Threolone (Chloramphenicol) is a broad-spectrum antibiotic that was derived from the bacterium Streptomyces venezuelae and is now produced synthetically. Threolone (Chloramphenicol) is effective against a wide variety of microorganisms, but due to serious side-effects (e.g., damage to the bone marrow, including aplastic anemia) in humans, it is usually reserved for the treatment of serious and life-threatening infections (e.g., typhoid fever). Threolone (Chloramphenicol) is bacteriostatic but may be bactericidal in high concentrations or when used against highly susceptible organisms. Threolone (Chloramphenicol) stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.

Prednisolone:


Pharmacological action

Threolone is a glucocorticosteroid (GCS). This medication inhibits the function of leukocytes and tissue macrophages. Threolone (Prednisolone) restricts the migration of leukocytes in the area of inflammation. This drug violates the ability of macrophages to phagocytosis and the formation of interleukin-1. Threolone (Prednisolone) contributes to the stabilization of lysosomal membranes, thereby reducing the concentration of proteolytic enzymes in inflammation. This medicine decreases capillary permeability caused by histamine release. Threolone (Prednisolone) inhibits the activity of fibroblasts and collagen formation.

Threolone (Prednisolone) inhibits the activity of phospholipase A2 which leads to suppression of the synthesis of prostaglandins and leukotrienes. This medication inhibits the release of COX (especially COX-2), which also helps reduce the production of prostaglandins.

Threolone (Prednisolone) reduces the number of circulating lymphocytes (T-and B-cells), monocytes, eosinophils and basophils as a result of their displacement from the bloodstream into lymphoid tissue; suppresses the formation of antibodies.

Threolone (Prednisolone) inhibits the release of pituitary ACTH and beta-lipotropina but it does not reduces the level of circulating beta-endorphin. This drug also inhibits the secretion of TSH and FSH.

Threolone (Prednisolone) has a vasoconstrictor effect with direct application to the vessels.

Threolone (Prednisolone) has a pronounced dose-dependent effect on the metabolism of carbohydrates, proteins and fats. It stimulates gluconeogenesis, amino acid contributes to the capture of the liver and kidneys and increases the activity of enzymes of gluconeogenesis. In the liver, Threolone (Prednisolone) enhances the deposition of glycogen by stimulating the activity of glikogensintetazy and synthesis of glucose from the products of protein metabolism. This medicine increases blood glucose activates the secretion of insulin.

Threolone (Prednisolone) inhibits glucose uptake by fat cells that leads to the activation of lipolysis. However, due to an increase in insulin secretion is stimulated lipogenesis which contributes to the accumulation of fat.

Threolone (Prednisolone) also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone Threolone (Prednisolone) affects the processes of water and electrolyte metabolism: promotes the excretion of potassium and calcium, delay in the body of sodium and water. Osteoporosis and Itsenko-Cushing's syndrome are the main factors limiting the long-term therapy with corticosteroids. As a result of the catabolic actions it may suppress growth in children.

In high doses prednisone can increase the excitability of brain tissue and contributes to lowering the threshold of convulsive readiness. This medication stimulates the excessive production of hydrochloric acid and pepsin in the stomach which leads to the development of peptic ulcers.

When systemic use the therapeutic activity of Threolone (Prednisolone) is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.

For external and local application the therapeutic activity of Threolone (Prednisolone) is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.

As compared with hydrocortisone the anti-inflammatory activity of Threolone (Prednisolone) is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.

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Pharmacokinetics

After oral administration Threolone (Prednisolone) is well absorbed from the gastrointestinal tract. Cmax in plasma observed after 90 min. In plasma most of Threolone (Prednisolone) is associated with transcortin (cortisol binding globulin). This drug metabolized primarily in the liver.

T1/2 is about 200 minutes.

Why is Threolone prescribed?

For oral and parenteral use: rheumatism; rheumatoid arthritis, dermatomyositis, periarteritis nodosa, scleroderma, ankylosing spondylitis, asthma, asthmatic status, acute and chronic allergic diseases, anaphylaxis, Addison's disease, acute adrenal insufficiency, adrenogenital syndrome; hepatitis, hepatic coma, hypoglycemic states, lipid nephrosis; agranulocytosis, various forms of leukemia, lymphoma, thrombocytopenic purpura, hemolytic anemia; chorea; pemphigus, eczema, pruritus, exfoliative dermatitis, psoriasis, pruritus, seborrheic dermatitis, SLE, erythroderma, alopecia.

For intra-articular administration: chronic arthritis, post-traumatic arthritis, osteoarthritis of large joints, rheumatic destruction of individual joints, arthritis.

For the introduction of infiltration in the tissue: epicondylitis, tenosynovitis, bursitis, frozen shoulder, keloids, sciatica, Dupuytren's contracture, rheumatism and similar lesions of joints and various tissues.

For use in ophthalmology: allergies, chronic and atypical conjunctivitis and blepharitis; inflammation of the cornea with intact mucosa; acute and chronic inflammation of the anterior segment of the choroid, sclera and episcleritis; sympathetic inflammation of the eyeball; after injuries and operations during prolonged stimulation of eyeballs.

Dosage and administration

When Threolone administered orally for replacement therapy in adults the initial dose is 20-30 mg, maintenance dose is 10.5 mg / day. If necessary, the initial dose is may be 15-100 mg / day, the maintenance one is 5-15 mg / day. The daily dose should be reduced gradually. For children the starting dose is 1-2 mg / kg in 4-6 receptions, the maintenance one is 300-600 mg / kg / day.

For IM or IV dose administration the multiplicity and duration of application are determined individually.

When intra-articular administration in large joints it used a dose of 25-50 mg, for medium-sized joints - 10-25 mg for small joints - 5-10 mg. For the introduction of infiltration into the tissues depending on disease severity and magnitude of the defeat use doses from 5 mg to 50 mg.

Threolone (Prednisolone) used topically in ophthalmology 3 times / day, course of treatment is no more than 14 days; in dermatology - 1-3 times / day.

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Threolone (Prednisolone) side effects, adverse reactions

Endocrine system: menstrual irregularities, suppression of adrenal function, Itsenko-Cushing's syndrome, suppression of pituitary-adrenal system, reduced tolerance to carbohydrates, steroid diabetes, or a manifestation of latent diabetes, growth retardation in children, delayed sexual development in children.

Digestive system: nausea, vomiting, steroid ulcer and duodenal ulcer, pancreatitis, esophagitis, bleeding and perforation of the gastrointestinal tract, increased or decreased appetite, flatulence, hiccups. In rare cases - elevated liver transaminases and alkaline phosphatase.

Metabolism: the negative nitrogen balance due to protein catabolism, increased excretion of calcium from the body, hypocalcemia, weight gain, increased sweating.

Cardiovascular system: the loss of potassium, hypokalemic alkalosis, arrhythmia, bradycardia (up to cardiac arrest); steroid myopathy, heart failure (the development or worsening of symptoms), ECG changes typical of hypokalemia, increased blood pressure, hypercoagulability, thrombosis. In patients with acute myocardial infarction - the spread of necrosis, slowing the formation of scar tissue that can lead to rupture of the heart muscle.

Musculoskeletal system: slowing growth and ossification processes in children (premature closure of epiphyseal growth zones) and osteoporosis (very rarely - pathological fractures, aseptic necrosis of the humeral head and femoral), rupture of tendons of muscles, muscle weakness, steroid myopathy, loss of muscle mass (atrophy).

CNS: headache, increased intracranial pressure, delirium, disorientation, euphoria, hallucinations, manic-depressive psychosis, depression, nervousness or anxiety, insomnia, dizziness, vertigo, pseudotumor cerebellum, and seizures.

Vision: the rear subcapsular cataracts, increased intraocular pressure (with the possible damage to the optic nerve), trophic changes of the cornea, exophthalmos, the propensity to develop secondary infections (bacterial, fungal, viral).

Dermatological reactions: petechiae, ecchymosis, thinning and fragility of the skin, hyper- or hypopigmentation, acne, stretch marks, susceptibility to the development of pyoderma and candidiasis.

Reactions due to immunosuppressive effect: slow process of regeneration, reduced resistance to infections.

For parenteral administration: in rare cases of anaphylactic and allergic reactions, hyper- or hypopigmentation, atrophy of skin and subcutaneous tissue, exacerbation after intrasinovialnogo applications such as Charcot arthropathy, sterile abscesses, when injected into pockets on the head - blindness.

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Threolone contraindications

For short-term use for health reasons - increased sensitivity to Threolone (Prednisolone).

For intra-articular injection and injection directly into the lesion: previous arthroplasty, abnormal bleeding (endogenous or caused by the use of anticoagulants), intra-articular fracture, infection (sepsis) inflammation in the joints and periarticular infections (including in history), as well as general infectious disease marked juxta-articular osteoporosis, lack of signs of inflammation in the joints ("dry" joint, such as osteoarthritis without synovitis), severe bone destruction and deformity of the joint (a sharp narrowing of joint space, ankylosis), the instability of the joint as a result of arthritis, aseptic necrosis of the epiphyses of bones forming the joint.

For external use only: bacterial, viral, fungal skin diseases, tuberculosis, skin, cutaneous manifestations of syphilis, skin tumors, post-vaccination period, violation of the integrity of the skin (ulcers, wounds), children's age (up to 2 years, with itching in the anal area - up to 12 years), rosacea, acne vulgaris, perioral dermatitis.

For use in ophthalmology: bacterial, viral, fungal eye diseases, tuberculosis eye disease, trachoma, violating the integrity of ocular epithelium.

Using during pregnancy and breastfeeding

During pregnancy Threolone (Prednisolone) is used only for health reasons. If necessary use of Threolone (Prednisolone) during lactation should carefully weigh the potential benefits of treatment for both mother and child at risk.

Special instructions

With care use for parasitic and infectious diseases of viral, fungal or bacterial origin - herpes simplex, herpes zoster (viraemic phase), chicken pox, measles, amoebiasis, strongyloidiasis, systemic mycosis, active and latent tuberculosis.

Be wary of up to 8 weeks before and 2 weeks after vaccination, and lymphadenitis after BCG, with immunodeficiency (including AIDS or HIV infection).

Be wary of diseases in gastrointestinal tract: gastric ulcers and duodenal ulcers, esophagitis, gastritis, acute or latent peptic ulcer, the newly created anastomosis intestinal ulcerative colitis with the threat of perforation or abstsedirovaniya, diverticulitis. Be wary of Threolone (Prednisolone) use in diseases of the cardiovascular system, including after recent myocardial infarction, with decompensated congestive heart failure, hypertension, hyperlipidemia, with endocrine diseases - diabetes mellitus, hyperthyroidism, hypothyroidism, pituitary basophilia, with severe chronic renal and / or liver failure, nefrourolitiaze, with hypoalbuminemia, with systemic osteoporosis, myasthenia gravis, acute psychosis, obesity III-IV stage, in poliomyelitis, open- and closed-angle glaucoma.

If necessary, intra-articular injection with caution in patients with severe general condition, failure (or brevity) of the 2 previous injections (with regard to individual properties apply GCS). During treatment (especially long-term) it needed to monitor at eye specialist, blood pressure control and water-electrolyte balance, and the pattern of peripheral blood glucose levels; to reduce the side effects can be assigned anabolic steroids, antibiotics, and increase the flow of potassium in the body (diet, potassium containing medications).

It is recommended to clarify the need for injection of ACTH after treatment with prednisone (after a skin test).

When Addison's disease should avoid the simultaneous use of barbiturates.

After cessation of treatment it may be experience a withdrawal syndrome, adrenal insufficiency and exacerbation of the disease, about which he was appointed Threolone (Prednisolone).

When intercurrent infections, septic conditions, and tuberculosis, must be simultaneous antibiotic therapy.

The children in the period of growth GCS should be used only if absolutely indicated and under close medical supervision.

Externally Threolone (Prednisolone) should not be used for more than 14 days. In case of application for ordinary or pink acne perhaps exacerbation.

Threolone drug interactions

Simultaneous administration of Threolone (Prednisolone) with:

  • salicylates may increase the likelihood of bleeding;
  • diuretics possible aggravation of violations of electrolyte metabolism;
  • hypoglycemic agents reduced the rate of decrease in blood glucose levels;
  • cardiac glycosides increases the risk of glycoside intoxication;
  • rifampin may weaken the therapeutic action of rifampicin;
  • antihypertensive drugs may reduce their effectiveness;
  • coumarin derivatives may weaken the anticoagulant effect;
  • rifampin, phenytoin, barbiturates, may weaken the effect of Threolone (Prednisolone);
  • hormonal contraceptives - strengthening of Threolone (Prednisolone);
  • acetylsalicylic acid may reduce the content of salicylates in blood;
  • praziquantel can reduce its concentration in the blood;
  • m-choline blockers (including antihistamines, tricyclic antidepressants), nitrate promotes increase in intraocular pressure;The appearance of hirsutism and acne it promotes the simultaneous use of other corticosteroids, androgens, estrogens, oral contraceptives, and anabolic steroid. The risk of developing cataracts increases with the use of corticosteroids against antipsychotic drugs, carbutamide and azathioprine.

    Threolone in case of emergency / overdose

    Risk of overdose increases with prolonged use of prednisone, particularly in large doses.

    Symptoms: increased blood pressure, peripheral edema, increased side effects of the drug.

    Treatment of acute overdose: an immediate gastric lavage or induction of vomiting, specific antidote is not found.

    Treatment of chronic overdose: should reduce the dose of the drug.

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    Threolone pharmaceutical active ingredients containing related brand and generic drugs:

    infoActive ingredient is the part of the drug or medicine which is biologically active. This portion of the drug is responsible for the main action of the drug which is intended to cure or reduce the symptom or disease. The other portions of the drug which are inactive are called excipients; there role is to act as vehicle or binder. In contrast to active ingredient, the inactive ingredient's role is not significant in the cure or treatment of the disease. There can be one or more active ingredients in a drug.


    Threolone available forms, composition, doses:

    infoForm of the medicine is the form in which the medicine is marketed in the market, for example, a medicine X can be in the form of capsule or the form of chewable tablet or the form of tablet. Sometimes same medicine can be available as injection form. Each medicine cannot be in all forms but can be marketed in 1, 2, or 3 forms which the pharmaceutical company decided based on various background research results.
    Composition is the list of ingredients which combinedly form a medicine. Both active ingredients and inactive ingredients form the composition. The active ingredient gives the desired therapeutic effect whereas the inactive ingredient helps in making the medicine stable.
    Doses are various strengths of the medicine like 10mg, 20mg, 30mg and so on. Each medicine comes in various doses which is decided by the manufacturer, that is, pharmaceutical company. The dose is decided on the severity of the symptom or disease.


    Threolone destination | category:

    infoDestination is defined as the organism to which the drug or medicine is targeted. For most of the drugs what we discuss, human is the drug destination.
    Drug category can be defined as major classification of the drug. For example, an antihistaminic or an antipyretic or anti anginal or pain killer, anti-inflammatory or so.


    Threolone Anatomical Therapeutic Chemical codes:

    infoA medicine is classified depending on the organ or system it acts [Anatomical], based on what result it gives on what disease, symptom [Therapeutical], based on chemical composition [Chemical]. It is called as ATC code. The code is based on Active ingredients of the medicine. A medicine can have different codes as sometimes it acts on different organs for different indications. Same way, different brands with same active ingredients and same indications can have same ATC code.


    Threolone pharmaceutical companies:

    infoPharmaceutical companies are drug manufacturing companies that help in complete development of the drug from the background research to formation, clinical trials, release of the drug into the market and marketing of the drug.
    Researchers are the persons who are responsible for the scientific research and is responsible for all the background clinical trials that resulted in the development of the drug.


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    References

    1. Dailymed."VICETON (CHLORAMPHENICOL) TABLET, COATED [OSBORN ]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
    2. Dailymed."PREDNISTAB (PREDNISOLONE) TABLET [LLOYD, INC. OF IOWA]". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).
    3. Dailymed."PREDNISOLONE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailym... (accessed August 28, 2018).

    Frequently asked Questions

    Can i drive or operate heavy machine after consuming Threolone?

    Depending on the reaction of the Threolone after taken, if you are feeling dizziness, drowsiness or any weakness as a reaction on your body, Then consider Threolone not safe to drive or operate heavy machine after consumption. Meaning that, do not drive or operate heavy duty machines after taking the capsule if the capsule has a strange reaction on your body like dizziness, drowsiness. As prescribed by a pharmacist, it is dangerous to take alcohol while taking medicines as it exposed patients to drowsiness and health risk. Please take note of such effect most especially when taking Primosa capsule. It's advisable to consult your doctor on time for a proper recommendation and medical consultations.

    Is Threolone addictive or habit forming?

    Medicines are not designed with the mind of creating an addiction or abuse on the health of the users. Addictive Medicine is categorically called Controlled substances by the government. For instance, Schedule H or X in India and schedule II-V in the US are controlled substances.

    Please consult the medicine instruction manual on how to use and ensure it is not a controlled substance.In conclusion, self medication is a killer to your health. Consult your doctor for a proper prescription, recommendation, and guidiance.

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    Review

    sDrugs.com conducted a study on Threolone, and the result of the survey is set out below. It is noteworthy that the product of the survey is based on the perception and impressions of the visitors of the website as well as the views of Threolone consumers. We, as a result of this, advice that you do not base your therapeutic or medical decisions on this result, but rather consult your certified medical experts for their recommendations.

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    The information was verified by Dr. Arunabha Ray, MD Pharmacology

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