The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Description: Alimemazine (Temaril P), a phenothiazine derivative, is an antihistamine w/ marked sedative and antiemetic effects. Additionally, it has antispasmodic, antiserotonin, and weak antimuscarinic properties.
Pharmacokinetics:
Absorption: Delayed by food. Bioavailability: <70%.
Distribution: Plasma protein binding: >90%.
Alimemazine (Temaril P) administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
May be taken with or without food.
Alimemazine (Temaril P) pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
Trimeprazine (also known as Alimemazine (Temaril P)) is a tricyclic antihistamine, similar in structure to the phenothiazine antipsychotics, but differing in the ring-substitution and chain characteristics. Trimeprazine is in the same class of drugs as chlorpromazine (Thorazine) and trifluoperazine (Stelazine); however, unlike the other drugs in this class, trimeprazine is not used clinically as an anti-psychotic. It acts as an anti-histamine, a sedative, and an anti-emetic (anti-nausea). Trimeprazine is used principally as an anti-emetic, to prevent motion sickness or as an anti-histamine in combination with other medications in cough and cold preparations. Tricyclic antihistamines are also structurally-related to the tricyclic antidepressants, explaining the antihistaminergic adverse effects of these two drug classes and also the poor tolerability profile of tricyclic H1-antihistamines.
Actions of Prednisolone (Temaril P) in details
The action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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Prednisolone (Temaril P) is a glucocorticosteroid (GCS). This medication inhibits the function of leukocytes and tissue macrophages. 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. Prednisolone (Temaril P) 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. Prednisolone inhibits the activity of fibroblasts and collagen formation.
Prednisolone (Temaril P) 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.
Prednisolone (Temaril P) 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.
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.
Prednisolone (Temaril P) has a vasoconstrictor effect with direct application to the vessels.
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, 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.
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.
Prednisolone (Temaril P) also has catabolic effects in lymphoid and connective tissue, muscle, adipose tissue, skin, bone tissue. To a lesser extent than hydrocortisone 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 prednisolone is due to anti-inflammatory, antiallergic, immunosuppressive and antiproliferative action.
For external and local application the therapeutic activity of prednisolone is due to anti-inflammatory, antiallergic and antiexudative (due to vasoconstrictor effect) effect.
As compared with hydrocortisone the anti-inflammatory activity of prednisolone is 4 times greater, the mineralocorticoid activity is 0.6 times smaller.
How should I take Prednisolone (Temaril P)?
Take Prednisolone (Temaril P) 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.
Your doctor may occasionally change your dose to make sure you get the best results.
Your steroid medication needs may change if you have unusual stress such as a serious illness, fever or infection, or if you have surgery or a medical emergency. Tell your doctor about any such situation that affects you.
Measure the liquid form of Prednisolone (Temaril P) with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
You may need to shake the Prednisolone (Temaril P) oral suspension (liquid) well just before you measure a dose. Follow the directions on your medicine label.
Keep the disintegrating tablet in its blister pack until you are ready to take the medicine. Open the package using dry hands, and peel back the foil from the tablet blister (do not push the tablet through the foil). Remove the tablet and place it in your mouth.
Allow the Prednisolone (Temaril P) orally disintegrating tablet to dissolve in your mouth without chewing. Swallow several times as the tablet dissolves. If desired, you may drink liquid to help swallow the dissolved tablet.
Steroids can cause you to have unusual results with certain medical tests. Tell any doctor who treats you that you are using Prednisolone (Temaril P).
Do not stop using Prednisolone (Temaril P) suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using Prednisolone (Temaril P).
Wear a medical alert tag or carry an ID card stating that you take Prednisolone (Temaril P). Any medical care provider who treats you should know that you take steroid medication.
Store Prednisolone (Temaril P) at room temperature away from moisture and heat.
Prednisolone (Temaril P) administration
Administration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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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.
Your doctor may occasionally change your dose to make sure you get the best results.
Your steroid medication needs may change if you have unusual stress such as a serious illness, fever or infection, or if you have surgery or a medical emergency. Tell your doctor about any such situation that affects you.
Measure the liquid form of prednisolone with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
You may need to shake the oral suspension (liquid) well just before you measure a dose. Follow the directions on your medicine label.
Keep the disintegrating tablet in its blister pack until you are ready to take the medicine. Open the package using dry hands, and peel back the foil from the tablet blister (do not push the tablet through the foil). Remove the tablet and place it in your mouth.
Allow the disintegrating tablet to dissolve in your mouth without chewing. Swallow several times as the tablet dissolves. If desired, you may drink liquid to help swallow the dissolved tablet.
Steroids can cause you to have unusual results with certain medical tests. Tell any doctor who treats you that you are using prednisolone.
Do not stop using prednisolone suddenly, or you could have unpleasant withdrawal symptoms. Ask your doctor how to avoid withdrawal symptoms when you stop using prednisolone.
Wear a medical alert tag or carry an ID card stating that you take prednisolone. Any medical care provider who treats you should know that you take steroid medication.
Store at room temperature away from moisture and heat.
Prednisolone (Temaril P) pharmacology
Pharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.
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Mechanism of Action
Naturally occurring glucocorticoids (hydrocortisone and cortisone), which also have salt-retaining properties, are used as replacement therapy in adrenocortical deficiency states. Their synthetic analogs such as prednisolone are primarily used for their potent anti-inflammatory effects in disorders of many organ systems.
Glucocorticoids such as prednisolone cause profound and varied metabolic effects. In addition, they modify the body's immune responses to diverse stimuli.
Prednisolone is a synthetic adrenocortical steroid drug with predominantly glucocorticoid properties. Some of these properties reproduce the physiological actions of endogenous glucocorticosteroids, but others do not necessarily reflect any of the adrenal hormones' normal functions; they are seen only after administration of large therapeutic doses of the drug. The pharmacological effects of prednisolone which are due to its glucocorticoid properties include: promotion of gluconeogenesis; increased deposition of glycogen in the liver; inhibition of the utilization of glucose; anti-insulin activity; increased catabolism of protein; increased lipolysis; stimulation of fat synthesis and storage; increased glomerular filtration rate and resulting increase in urinary excretion of urate (creatinine excretion remains unchanged); and increased calcium excretion.
Depressed production of eosinophils and lymphocytes occurs, but erythropoiesis and production of polymorphonuclear leukocytes are stimulated. Inflammatory processes (edema, fibrin deposition, capillary dilatation, migration of leukocytes and phagocytosis) and the later stages of wound healing (capillary proliferation, deposition of collagen, cicatrization) are inhibited.
Prednisolone can stimulate secretion of various components of gastric juice. Suppression of the production of corticotropin may lead to suppression of endogenous corticosteroids. Prednisolone has slight mineralocorticoid activity, whereby entry of sodium into cells and loss of intracellular potassium is stimulated. This is particularly evident in the kidney, where rapid ion exchange leads to sodium retention and hypertension.
Pharmacokinetics
Absorption
The maximum serum concentration of Prednisolone (Temaril P) occurs within 1 to 2 hrs following a single dose of oral administration. Food intake prolongs the time to peak concentration, but does not affect the extent of absorption significantly.
Distribution
Prednisolone is reported to be 70-90% protein-bound in the plasma and the volume of distribution is reported as 0.22 - 0.7 L/kg.
Metabolism
Prednisolone is reported to be metabolized mainly in the liver and excreted in the urine as sulfate and glucuronide conjugates.
Excretion
Prednisolone (Temaril P) is eliminated from the plasma with a half-life of 2 to 3 hours.
Oral administration of single dose of 15 mg/5 mL of Prednisolone (Temaril P), 15 mg/5 mL Prednisolone USP syrup, and 3× 5 mg Prednisolone USP tablets in 24 adult volunteers yielded comparable pharmacokinetic data:
Table 1. Comparison of Mean Pharmacokinetic Parameters (%CV) in Healthy Volunteers Following a Single Dose of 15 mg/5 mL of Prednisolone (Temaril P), 15 mg/5 mL Prednisolone USP Syrup, and 3× 5 mg Prednisolone USP Tablets
Dose*
(15 mg prednisolone base equivalent)
AUC0-∞ (ng∙hr/mL)
(%CV)
Cmax (ng∙hr/mL)†
(%CV)
*
Administered under fasting conditions.
†
Mean values of 24 normal volunteers.
Prednisolone (Temaril P) Suspension
1999.4 (60.0)
321.1 (52.0)
Prednisolone Syrup
1872.7 (50.4)
362.4 (37.8)
Prednisolone Tablet
1968.4 (54.6)
326.9 (43.5)
The systemic availability, metabolism and elimination of prednisolone after administration of single weight-based doses (0.8 mg/kg) of intravenous (IV) prednisolone and oral prednisone were reported in a study of 19 younger adult (aged 23 to 34 years) and 12 geriatric (65 to 89 years) subjects. Results showed that the systemic availability of total and unbound prednisolone, as well as interconversion between prednisolone and prednisone were independent of age. The mean unbound fraction of prednisolone was higher, and the steady-state volume of distribution (Vss) of unbound prednisolone was reduced in elderly patients. Plasma prednisolone concentrations were higher in elderly subjects, and the higher AUCs of total and unbound prednisolone were most likely reflective of an impaired metabolic clearance, evidenced by reduced fractional urinary clearance of 6b-hydroxyprednisolone. Despite these findings of higher total and unbound prednisolone concentrations, elderly subjects had higher AUCs of cortisol, suggesting that the elderly population is less sensitive to suppression of endogenous cortisol or their capacity for hepatic inactivation of cortisol is diminished.
References
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/dailyme... (accessed September 17, 2018).
NCIt. "Prednisolone: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
EPA DSStox. "Prednisolone: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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