Outline:Glucocorticoid is a hormonal secretion of gland adrenal medulla and has important effects on body like carbohydrate, fat and protein metabolism, immunological response and on inflammation. They act on glucocorticoid receptor which is present in almost every tissue in human body.
Triamcinolone acetonide is a synthetic glucocorticoid with the molecular formula of C24H31FO6 and molecular weight 434.51. They are used as anti-inflammatory, immunosuppressive and anti-itch agent in clinics.
Triamcinolone acetonide also contains some inactive substances in their formulation some are mention below:
- Benzyl alcohol
- Wax- emulsifying
- Lactic acid
- Water – purified
- Isopropyl palmitate
The potency of topical formulations are of high or medium.
They act on their receptors which are present in cytosole and then translocate this receptor-ligand complex into the nucleus then interact with DNA and change the gene expression. They prevent the synthesized of leukotrienes and prostaglandins by blocked the released of arachidonic acid by inhibit the lipocortins. They also the suppressed the formation of pro-inflammatory substance like, interleukin(IL)-1 and IL-6 and also decreases the circulating lymphocytes, they all are the mediator of inflammation thus from this action of mechanism they suppressed the anti-inflammatory responses.
Anti-inflammatory effects of triamcinolone is occurred by inhibit the movement of macrophages and leukocytes towards the inflamed area, these effects reduced the possibility of edema, erythema, pruritus, and degeneration of the skin.
In asthamic condition it will act by delayed the allergic reaction to certain allergens. And also beneficial in acute attack of asthma but inhaled triamcinolone does not have bronchodilated properties. In short it reduces the action of chemical which provoked the inflammation.
It works by activating natural substances in the skin to reduce the sign and symptoms. They are available in oral, parenteral by intramuscularly, topical (ointment, lotion, cream, paste, topical aerosol) and aerosol by inhalation, forms . Triamcinolone acetonide accept by FDA (food and drug administration) in 1957
They are used for following purposes:
- Perennial and seasonal allergic rhinitis
- Nephrotic syndrome
- For anti-itching agent
- Acute gouty arthritis
- Lupus erythematous
- Hemolytic anemia
- Acne vulgaris
- Alopecia (hair loss)
- Rheumatic fever
- Rheumatic arthritis
- Chron’s disease
- nappy rash
- Edema of the cerebrum associated with primary or metastatic brain tumor.
- Keloid scars
- Lichen planus (LP)
- Necrobiosis lipoidica diabeticorum
- Mycosis fungoides (MF)
- Post hepatic neuralgia (PHN)
- Secondary adrenocortical insufficiency (SAI)
- Idiopathic eosinophilic pneumonias
- Ocular inflammatory conditions
- Severe erythema multiforme
- Symptomatic sarcoidosis
- Granuloma annulare lesions
- Cystic tumor of the ganglia
- Acute theumatic heart disease, unspecified
- Acute bursitis
- Ulcerative colitis
- Tuberculosis infection
- Pure red cell aplasia
- Termination of pregnancy of 13-24 weeks gestation.
- Acute multiple sclerosis.
- Endocrine disorder.
- Nonspecific tenosynovitis.
- Mouth sores
And for all type of anti-inflammatory and allergic disorders.
Pharmacokinetics: pharmacokinetics is a branch of pharmacology which deals with the movement of drug with in the human body for example: drug absorption, distribution, metabolism and elimination. It is necessary for the drug to produce their effects. Topical form is readily absorbed from the intact skin, blisters, inflammation or any cracks in skin increased the absorption time
Absorption: absorption are rapid through IV route followed by oral administration.
Topical route is also fast as compared to others drug.
Volume of distribution: volume of distribution is 103L. if it applied topically the distribution is throughout the local skin layer. Drug also distributed in intestion, muscle, liver, skin, kidneys, breast milk and across the placenta.
Protein binding: protein binding is 68%. It is constant, predictable, and relatively low. Only the unbound portion of drug is active.
Drug administration: it is administrated by orally, topically, inhaled by spray, nasal, intra muscular, intra- articularly or via intra vitreal.
Oral route: for oral route suspensions, solutions, and tablets are available.
Once absorbed through the mucous membrane of oral mucosa the effects of drug is same as systemic administrated drug.
IM route: single IM dose of 40-60mg within 24 to 48 hours and then returns to normal usually in 30 to 35 days.
Topical route: absorption through the skin is depend on the condition of the skin, absorption increases in inflamed or cracked skin or at thin skin site like face genital skin and eyelids.
Inhalation route: absorption by the inhalation route is as same as GIT route.
Nasal route: dose below 440 mcg/day does not produce any therapeutics effects.
Intra – articular route: it is administrated through injection and may be absorbed systemically.
Metabolism: drug is mostly metabolized by skin and little bit metabolism occurred by liver which is absorbed in into systemic circulation, hepatic metabolism converted the drug into inactive compounds.
Route of elimination: inactive compounds of drugs are glucuronides and sulfates. Which are primarily excreted by kidneys. Little bit also excreted through faeces.
Some inactive metabolites of triamcinolone also excreted in bile.
Half life: half-life is the time required for the amount of drug in the body or systemic circulation to fall by 50%. The half-life of this drug is about 88 minutes.
Toxicity: lethal dose=> 500 mg/ kg (in rats)
Do not this medication for the longer period because of its worst side effects.
Topically applied triamcinolone overdose usually does not produce the life – threatening effects.
Affected organism: toxic affects seen on humans and other rodents.
Pharmacodynamics: pharmacodynamics is also the branch of pharmacology it deal with the drug action on the body. For example its effect and mechanism of action on the body function. It define the response if the body to the specific drug. It include the receptor and drug binding site on receptor.
Receptor: they bind with glucocorticoid receptor in cytosole.
The type of receptor is protein.
Dosage: therapeutic dose is that dose which produce the desired effect without any toxicity.
Injectable suspension: 10 mg/ml of kanalog-10 for intra-lesional or intra-articular indication.
Dilute with local anesthetic before intra-articular or intralesional injection. Avoid diluents containing parabens or phenols.
For the treatment of rhematic arthritic: 60 mg IM after every six weeks.
For the treatment of dermatoses: intralesional injection 1 mg per site or more times if needed but no exceed 30 mg/ day
For inflammatory and allergic conditions:60 mg/ IM injection. Range between 40-80 mg.
For multiple sclerosis: 160 mg IM per day for week.
Drug should be store at room temperature (59-86F). protect it from freezing temperature.
Maximum dose: the maximum dose of triamcinolone actenoid depend on the severity of disease, condition of patient and route of administration and response of the patient to the drug.
Precaution in dosing: liver impairment: therapeutic dose must be considered in various liver problem which decreased the liver function.
Renal impairment: not significance because it will eliminated through fecal route.
Side-effects: side effects are seen when drug is applied or used for the longer period of the time or sometime when high dose is used.
Increase glucose level, glycosuria, pruritus( itching), dryness, erythema, folliculitis, acneiform, perioral dermatitis, atrophy, hypopigmentation, steroid purpura, skin fragility, cushing’s syndrome, growth and adrenal reduction, acne hirsutism, glaucoma, buffalo bump, arrhythmias, mental depression, blurred vision, beating in the ears, breathlessness, swelling in extremities, trouble in thinking, speaking and walking, tingling sensation in the arms or legs moon face ,menstrual irregularity, blood, black and tarry stool, loss of libido, muscle pain, wasting or weakness, weight loss due to diarrhea and vomiting, thinning of your skin, full or bloated feeling small, red , or purple spots on the skin called petechiae , ocular hemorrhage, retinal detachment, papilledema, thromboembolism, pulmonary edema, cardiomyopathy, wheezing, constipation, blisters if dressing and bandages are used over the treated area and hypertension. They are less frequently occur in topically applied drug.
Effects of various laboratory tests:
It increases blood sugar level by stimulating the gluconeogenesis, lipolysis, protein catabolism and induce the secretion of insulin reduce the sensitivity of the cells to insulin. There-fore glucose concentration increases in the blood and became the cause of the increase blood sugar levels. Also reduces the peripheral uptake of glucose at the level of the adipose tissue and muscle level.
Drug interaction: drug interaction is the effect which is produce by two or more drugs when they administrated at the same period, and produce less effect if they would administrate separately, the resulting effect is depend on the drug type they may enhanced the drug activity or reduced it or may produce the unwanted side effects. Before using this drug tell your doctor about all the drugs which your using at that time.There are many drugs which interacted with triamcinolone acetonide some major, some moderate and some are minorly interacted. The drugs which are frequently interact with triamcinolone is aspirin, omega-3 polyunsaturated fatty acids, furosemide, metoprolol succinate ER, polyethylene glycol 3350, acetaminophen
Deterrent: it should be remembered that triamcinolone acetonide would be dangerous for the patient with hepatic, renal, cardiac and gastrointestinal tract diseases, hypertension, myasthenia gravis, diabetic mellitus and osteoporosis. Keep out of reach of children.
Contraindications: contraindications means the drug should not be used because it may be harmful for the person. Triamcinolone acetnoide is contraindicated in several conditions like diabetic mellitus because it increases the blood sugar level, fungal and bacterial infection, knonw hypersensitive patient, idiopathic thrombocytopenia purpura , psychosis patient, rosacea, myopathy, gravitational ulceration, acne vulgaris, osteoporosis, intestinal infection caused by the round worms, insufficiency of the hypothalamus and pituitary gland, immunosuppressive patients, low amount of potassium In the blood, inherent deficiency of arginosuccinate lyase and carbmyl phosphate synthetase, stomach ulcers, chicken pox or herpes infection (including cold sores) muscle weakness, malaria,exposure to the measles, muscle pain or tenderness, citrullinemia.
Consequences of drug abuse: addiction of the drug until it produced the life threating side effects is called drug abuse. There is no any history of drug abuse with triamcinolone acetnoide.
Long term effects of triamcinolone acetnoide: longer period of used may result in increase intra ocular pressure which leads to glaucoma and cataracts.
Precautions: avoid the drug if infection or symptoms of diseases persists or worsen. Triamcinolone suspension form is only intra muscular or intra articular and not for intra venous, epidural or intra thecal.
Neonates are contraindicated for triamcinolone
Prohibited in pregnancy, harm full for fetus in 1st trimester
The high dose of triamcinolone may increase mortality in patient with cephalic injury.
Cause muscle wasting.
Dangerous in renal insufficiency.
Not used in patient with diverticulitis.
In liver cirrhosis patient it will be harm full.
Caution in patient with autoimmune diseases like systemic lupas erythema and myasthenia gravis.
Avoided in hypertensive patient.
harm full in hypothyroidism.
It may enhance the psychiatric disorder like depression, euphoria, or personality changes.
In cushing syndrome.
In patient who have increased risk of getting infection.
It may kill or destroyed the vaccine therefore response of such vaccines cannot be revealed.
Epidural used is strickly prohibit because of its worst outcomes.
Caution in lactating mother because it excreted in breast milk.
Use precaution if used in face or body folds.
This drug should not be used by any children or adult below 18 years old unless your doctor prescribed it. Consult your doctor if there is any infection or inflammation at the site of drug application.
How many times used in day: it should be applied on affected area two to three times daily.
How to use triamcinolone:
Covered the affected area with the fine layer of drug it may worsen the inflammation or produce blisters. Do not rub and stretch the area. Do not covered the affected area with any bandage unless your doctor tells you to.
For mouth sores it applied in bed time usually after meal.
rinse your hands thoroughly with warm water, Avoid your eyes.
If dose is missed: administrate the missed dose as soon as possible but if the time of next dose is nearer then avoid the missed dose. do not use extra medicine to compensate the missed dose.
What should be avoided during drug therapy of triamcinolone: avoid using medicated skin products like face wash, creams which including alcohol, lime or astrigents.
Brand names: they came in market in) following names.
• Kenalog (dental paste
Veterinary use: it is often used in veterinary clinics as aerosol spary or topical ointment for the control of itching, inflammation and swelling in dogs and cats. In farms it is also use as pre inducer of birth in cows and goats for the purpose of contractions.
Side effects in dogs:
- Weight gain
- Loss of appetide or excessive eating
- Frequent urination
- Decrease immune system function
- Aggression or behavioural changes