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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Pharmacology: Preclinically, Ambroxol (Lovarin Ex) hydrochloride, the active ingredient of Ambroxol (Lovarin Ex), has been shown to increase respiratory tract secretion. It enhances pulmonary surfactant production and stimulates ciliary activity. These actions result in improved mucus flow and transport (mucociliary clearance). Improvement of mucociliary clearance has been shown in clinical pharmacologic studies. Enhancement of fluid secretion and mucociliary clearance facilitates expectoration, and eases cough.
In patients suffering from COPD, long-term treatment (6 months) with Ambroxol (Lovarin Ex) (Ambroxol (Lovarin Ex) Retard Capsule 75 mg) resulted in a significant reduction of exacerbations that became evident after 2 months of treatment. Patients in the Ambroxol (Lovarin Ex) treatment group lost significantly fewer days through illness and had fewer days when they needed antibiotic therapy. Treatment with Ambroxol (Lovarin Ex) Retard also induced a statistically significant improvement of symptoms (difficulty of expectoration, cough, dyspnea, auscultatory signs) compared with placebo.
A local anaesthetic effect of Ambroxol (Lovarin Ex) hydrochloride has been observed in the rabbit eye model which may be explained by the sodium-channel blocking properties. It was shown in vitro that Ambroxol (Lovarin Ex) hydrochloride blocks cloned neuronal sodium channels; binding was reversible and concentration-dependent.
Cytokine release from blood but also tissue-bound mononuclear and polymorphonuclear cells was found to be significantly reduced by Ambroxol (Lovarin Ex) hydrochloride in vitro.
In clinical studies in patients with sore throat, pharyngeal pain and redness was significantly reduced.
Following the administration of Ambroxol (Lovarin Ex), antibiotic concentrations (amoxicilline, cefuroxime, erythromycin) in bronchopulmonary secretions and in the sputum are increased.
Pharmacokinetics:Absorption: Absorption of all immediate release oral forms of Ambroxol (Lovarin Ex) hydrochloride is rapid and complete, with dose linearity in the therapeutic range. Maximum plasma levels are reached within 1 to 2.5 hours following oral administration of the immediate-release formulation and after a median of 6.5 hours of the slow-release formulation. The absolute bioavailability after a 30 mg tablet was found to be 79%. The slow-release capsule showed a relative availability of 95% (dose-normalized) in comparison to a daily dose of 60 mg (30 mg twice daily) administered as immediate-release tablet.
Distribution: In the therapeutic range, plasma protein-binding was found to be approximately 90%. Distribution of Ambroxol (Lovarin Ex) hydrochloride from blood to tissue is rapid and pronounced, with the highest concentration of the active substance found in the lungs. The volume of distribution following oral administration was estimated to be 552 L.
Metabolism and Elimination: About 30% of an orally administered dose is eliminated via first-pass metabolism.
Studies in human liver microsomes have shown that CYP3A4 is responsible for the metabolism of Ambroxol (Lovarin Ex). Ambroxol (Lovarin Ex) hydrochloride is metabolized primarily in the liver by glucuronidation and some cleavage to dibromanthranilic acid (approximately 10% of dose) aside from some minor metabolites.
Ambroxol (Lovarin Ex) hydrochloride is eliminated with a terminal elimination half-life of approximately 10 hours. Total clearance is in the range of 660 mL/min, with renal clearance accounting for approximately 83% of the total clearance.
Special Populations: In patients with hepatic dysfunction, elimination of Ambroxol (Lovarin Ex) hydrochloride is reduced, resulting in approximately 1.3 to 2-fold higher plasma levels.
Due to the high therapeutic range of Ambroxol (Lovarin Ex) hydrochloride, dose adjustments are not necessary.
Others: Age and gender were not found to affect the pharmacokinetics of Ambroxol (Lovarin Ex) hydrochloride to a clinically relevant extent and thus there is no necessity for adjustment of dosage regimens.
Food was not found to influence the bioavailability of Ambroxol (Lovarin Ex) hydrochloride.
Ambroxol (Lovarin Ex) 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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Should be taken with food.
Ambroxol (Lovarin Ex) 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.
When Max Pidek Pharmaceuticals administered orally amoxicillin rapidly and completely absorbed from the gastrointestinal tract and is not destroyed in the acidic environment of the stomach. Cmax of amoxicillin in the blood plasma is reached after 1-2 h. When increasing doses of 2 times the concentration also increased by 2 times. In the presence of food in the stomach does not reduce the overall removals. Similar concentrations of amoxicillin reached in the blood when administered orally, IV and IM.
The binding of amoxicillin to plasma proteins is about 20%.
Widely distributed in tissues and body fluids. Reported high concentrations of amoxicillin in the liver.
T1/2 from the plasma is 1-1.5 h. About 60% of the dose adopted by mouth, is excreted unchanged in the urine by glomerular filtration and tubular secretion, with a dose of 250 mg of amoxicillin concentration in urine exceeds 300 micrograms / ml. A number of amoxicillin is determined in feces.
T1/2 for Newborns and the elderly can be longer.
In renal insufficiency T1/2 may be 7-20 hours.
In small quantities amoxicillin penetrates through BBB in inflammation of the pia mater.
amoxicillin is removed by hemodialysis.
Actions of Loratadine (Lovarin Ex) 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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Pharmacology:Loratadine (Lovarin Ex) like other antihistamines acts via competitive blocking of H1-histaminic receptors. Loratadine (Lovarin Ex) penetrates very poorly into CNS. Therefore, it is devoid of significant CNS depressant effects. Loratadine (Lovarin Ex) is highly selective antagonist of H1-histaminic receptors. Loratadine (Lovarin Ex) has very weak affinity for α-adrenoreceptors or acetylcholine receptors. In animal models, Loratadine (Lovarin Ex) has very high affinity for H1-histaminic receptors, which is greater than that of the terfenadine or astemizole. The antihistaminic effect persists for 18-24 hrs. In human subjects, Loratadine (Lovarin Ex) suppresses wheal response to intradermally injected histamine. This action starts within 1-2 hrs of oral administration and maximum inhibitory effect evident in 2-4 hrs. The magnitude and duration of effects are dependent upon Loratadine (Lovarin Ex) dose. On long-term administration, the drug retains its effectiveness without developing tachyphylaxis. In animal models, Loratadine (Lovarin Ex) has also shown anti-serotonin activity. It also suppresses mast cell mediator release.
In addition, Loratadine (Lovarin Ex) also possess anti-allergic activity which has been demonstrated in humans by skin prick and nasal challenge tests.
In human volunteers, Loratadine (Lovarin Ex) did not reduce psychomotor performance as measured by sleep latency, symbol copying, digit symbol substitution, dynamic visual activity test or driving performance. In addition, Loratadine (Lovarin Ex) does not potentiate the effects of centrally acting drugs eg, diazepam, ethanol and barbiturates.
Pharmacokinetics: Absorption: In humans, Loratadine (Lovarin Ex) is rapidly absorbed after oral administration. There is a linear relationship between Loratadine (Lovarin Ex) dose and both Cmax and AUC. The 10, 20 and 40 mg of Loratadine (Lovarin Ex) produce peak plasma concentrations of 5, 11, 28 mcg/L, respectively. Time to reach maximum concentration occurs between 1-1.5 hrs. After repeated dosing steady-state plasma concentrations occur by 5th day.
Metabolism: Loratadine (Lovarin Ex) is metabolized to descarboethoxyloratadine (DCL) which is pharmacologically active.
Distribution: Loratadine (Lovarin Ex) has extensive distribution in the body. The distribution t½ of Loratadine (Lovarin Ex) and DCL is 1.02 and 3.8 hrs, respectively.
Loratadine (Lovarin Ex) is 97-99% bound to plasma proteins whereas DCL is 73-76% bound to plasma proteins. Small amount of both Loratadine (Lovarin Ex) and DCL is secreted in breast milk, but the amount is minimal.
Elimination: Loratadine (Lovarin Ex) undergoes extensive biotransformation. The elimination t½ of Loratadine (Lovarin Ex) after single dose is 8-11 hrs and that of DCL is 17-24 hrs. After multiple dosing, elimination t½ of Loratadine (Lovarin Ex) is 4.4 hrs and that of DCL is 8.7 hrs.
Pharmacokinetics of Loratadine (Lovarin Ex) and that of DCL is not affected in patients with renal disease and in plasma patients on hemodialysis. In elderly patients too, disposition kinetics of Loratadine (Lovarin Ex) and DCL is not affected. In patients of alcoholic liver disease, the t½ of Loratadine (Lovarin Ex) and that of DCL are longer but still within the range observed in a population of normal subjects.
How should I take Loratadine (Lovarin Ex)?
Use exactly as directed on the label, or as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended.
Loratadine (Lovarin Ex) is usually taken once per day. Follow your doctor's instructions.
Do not crush, chew, or break the regular Loratadine (Lovarin Ex) tablet. Swallow the pill whole.
Measure liquid medicine with a special dose-measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
To take Loratadine (Lovarin Ex) orally disintegrating tablet (Loratadine (Lovarin Ex), Alavert):
Keep the tablet in its blister pack until you are ready to take the medicine. Open the package and peel back the foil from the tablet blister. Do not push a tablet through the foil or you may damage the tablet.
Using dry hands, remove the tablet and place it on your tongue. It will begin to dissolve right away.
Do not swallow the tablet whole. Allow it to dissolve in your mouth without chewing.
Swallow several times as the tablet dissolves. If desired, you may drink water to help swallow the dissolved tablet.
Call your doctor if your symptoms do not improve.
Store at room temperature away from moisture and heat.
Loratadine (Lovarin Ex) 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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May be administered without regard to meals.
Dispersible tablet: Place in mouth and allow to dissolve. Swallow with or without water.
Loratadine (Lovarin Ex) 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.
Loratadine (Lovarin Ex) is a long acting second generation antihistamine that is similar in structure to cyproheptadine and azatadine. The pharmacology of Loratadine (Lovarin Ex) is similar to other antihistamines, but unlike other H1-blockers, loratidine is shown to exhibit competitive, specific, and selective antagonism of H1 receptors. The exact mechanism of this interaction is unknown, but disposition of the drug suggests that Loratadine (Lovarin Ex)'s prolonged antagonism of histamine may be due to the drug's slow dissociation from the receptor or the formation of the active metabolite, desloratadine. Loratadine (Lovarin Ex) does not penetrate the CNS effectively and has a low affinity for CNS H1-receptors.
References
DailyMed. "LORATADINE; PSEUDOEPHEDRINE SULFATE: 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. "Loratadine: 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. "Ambroxol: 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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