Pharmacology -5 Drugs - Assessment Answer

Pharmacology Assignment

Assignment Task

Introduction

Pharmakinetics

Drug group: Calcium Channel Blockers

Absorption: The medication is completely absorbed after the oral administration from the gastrointestinal tract and undergoes the extensive first pass effect (Lehne, & Rosenthal, 2014). The absorption of the medication begins in one hour with the maximum plasma concentration is achieved in 4 to 6 hours of administration (Lehne, & Rosenthal, 2014).

Distribution: the medication is distributed to the blood vessels in order to relax the blood vessels and improve the blood flow (Lehne, & Rosenthal, 2014).

Metabolism: The medication undergoes significant metabolism. The extensive metabolism occurs and only 2% to 4% of the drug passes through the urine (Lehne, & Rosenthal, 2014). Drugs which induce or inhibit hepatic microsomal enzymes may alter diltiazem disposition.

Excretion: Due to metabolism only 2% to 4% unchanged drug is excreted through urine (Lehne, & Rosenthal, 2014).

Pharmacodynamics

How does the drugs work?It works by relaxing the muscles of the blood vessels and the heart. This is a calcium channel blocker that helps in relaxing the blood vessels (Ettehad et al, 2016).

Side effects: weakness, dizziness, light-headedness, constipation, nausea and flushing may occur as side effects (Hodgson & Kizior, 2012).

Precautions: Must be carefully used in the patients with the history of any kind of allergies. Must also be carefully used in patients with kidney, liver and lung disorders (Hodgson & Kizior, 2012).

Uses: The drug is mainly used to control the blood pressure in the patients suffering with high blood pressure. Drug can also be used to treat chest pain (angina) (Hodgson & Kizior, 2012). Also, it is used to prevent the chances of stroke. Increase ability to exercise by reducing chest pain.

Conversyl

Pharmakinetics

Drug group: angiotensin converting enzyme (ACE) inhibitors.

Absorption: After the oral administration of the drug, it is considered to be quickly absorbed and also displays the bioavailability of 24% (Lehne, & Rosenthal, 2014). The drug is mainly eliminated through urine and the half-life of plasma is approximately 1 hour (Lehne, & Rosenthal, 2014). Bioavailability of the active metabolite perindoprilat is approximately 27% (Product information, 2018).

Distribution:the peak plasma concentration of the perindoprilat occurs after the 3-4 hours of the oral administration of Conversyl (Lehne, & Rosenthal, 2014). The protein binding of the perindoprilat is 20% (Product information, 2018).

Metabolism: Apart of perindoprilat, the administration of the medication give rise to five different kind of metabolites. However, all of them are inactive and are present in very low quantity (Lehne, & Rosenthal, 2014). The hepatic first pass effect results in the development of glucuronoconjugate of perindoprilat. However, biotransformation of perindoprilat can be reduced by the food intake (Product information, 2018).

Excretion: In the process of elimination firstly Perindoprilat binds to the plasma and tissue ACE (Product information, 2018). After this binding, Perindoprilat that is left free is eliminated through urine (Product information, 2018).

Pharmacodynamics

How does the drugs work?It is used to treat high blood pressure, as it helps in lowering blood pressure by soothing down the blood vessels (Greenstein, 2017).

Side effects: Some of the common side effects may include persistent dry cough, diarrhoea, difficulty in maintaining erection headache, dizziness, swelling in hands, legs and feet and loss of taste (Greenstein, 2017).

Precautions: Medical attention should be given in the case of swelling in face, tongue and glottis. Can affect the sugar control in diabetes patients, therefore, special monitoring is required (Greenstein, 2017).

Uses: The drug is mainly used to treat the problem of high blood pressure after the heart attack or stroke. It is also used to treat congestive heart failure (Greenstein, 2017).

Lasix

Pharmakinetics

Drug Group: Furosemide loop diuretic

Absorption: The drug is absorbed quickly after the administration of Lasix in the duodenum in humans. The peak plasma concentration of the drug is reached in 1 hour. The peak concentration is higher by the direct administration in the duodenum (Van Wart et al, 2014).

Distribution: it binds strongly with the anionic binding sites on albumin and display very negligible binding to the protein of the tissue (Van Wart et al, 2014).

Metabolism: The location of the metabolism is probenecid. 85% of the total clearance is through kidney (Van Wart et al, 2014).

Excretion: The amount of the unchanged furosemidein the urine is higher when the administration of the medication is direct in duodenum (Brenes-Salazar et al 2015)

Pharmacodynamics

How does the drugs work?This drug blocks the absorption of the sodium, chloride and water from the fluid that is filtered in the kidney tubules. This process of drug results in increasing the output of urine (Brenes-Salazar et al, 2015).

Side effects: Some of the serious side effects of the drug include, pancreatitis, jaundice, oral and gastric irritation, diarrhoea, constipation, nausea and vomiting (Brenes-Salazar et al, 2015).

Precautions: The therapy of drug should be continued till the condition improves. Sudden alteration in the fluid and electrolyte balance should be avoided. Excessive diuresis can result in dehydration (Opsha, 2016).

Uses: Mainly used for removing excessive fluid from the body, which had resulted because of the condition of stroke, heart attack and kidney disorder. Also used for lowering high blood pressure (Opsha, 2016).

Aspirin

Pharmakinetics

Drug Group: nonsteroidalanti-inflammatory drug (NSAID).

Absorption: Aspirin is administered orally and absorbed in the gastrointestinal tract of the human body (Patrick et al, 2015).

Distribution: The drug is distributed to all the tissues and fluid inside the body. At the low concentration oapproximately 90% of plasma sacylate is bound to albumin, while in higher concentration it is only 75% (Hodgson, & Kizior, 2012).

Metabolism: metabolism of80% of takes place in the liver. The metabolism mainly occurs due to the hepatic conjugation with glycin to form salicyluric acidand it can also metabolise with glucuronic acid to form salicyl acyl and phenolic glucuronide (Patrick et al, 2015).

Excretion:75% of the drug is excreted through kidney in the form of salicyluric acid (Hodgson, & Kizior, 2012).

Pharmacodynamics

How does the drugs work?Aspirin works by reducing the production of thromboxane that is significant for preventing heart attack and strokes (Hodgson, & Kizior, 2012).. Thromboxane is a chemical that is responsible for the thickening of the platelets. When the drug works less thromboxane is made by platelets and therefore, less likely to form the clot in the blood vessel (Paez Espinosa, Murad, & Khasawneh, 2011).

Side effects: The common side effects are heartburn and upset stomach. Some of the serious side effects could be easy bruising, ringing in the ears, difficulty in hearing, and kidney problems (Hodgson, & Kizior, 2012).

Precautions: Patient with any kind of allergies must avoid aspirin Precautions should be taken in case of patients with kidney, liver, stomach problems and also if patient have asthma (Hodgson, & Kizior, 2012).

Uses: Mainly used in relieving moderate fever and preventing mild to moderate pain. Given to the patients to stroke patient to reduce the formation of blood clot (Paez Espinosa, Murad, & Khasawneh, 2011).

Tissue Plasminogen activator

Pharmakinetics

Drug Group: thrombolytic drugs

Absorption: Administered intravenous and it is mainly formed by the recombinant DNA and mainly binds to fibrin and works in converting plasminogen to plasmin (Hodgson & Kizior, 2012).

Distribution: it helps in dissolving the blood clots by activating plasminogen. It is extensively distributed in the body tissues (Hodgson & Kizior, 2012).

Metabolism: Metabolism of the drug is poorly understood, but mainly it is hepatic and mainly occurs with hepatocytes (Hodgson & Kizior, 2012).

Excretion: it undergoes renal elimination with the half life of 90-130 minutes (Hodgson & Kizior, 2012)

Pharmacodynamics

How does the drugs work?The drug is administered directly to the blood vessel and the high concentration of tPA build up on the site of the clot, helps in dissolving the clot and improves the blood flow to the brain (Hodgson & Kizior, 2012).

Side effects: side effects of the drug can include bleeding from the wounds and puncture sites, bleeding gums, blood coming in cough, difficulty in swallowing and breathing, headache and dizziness (Lehne & Rosenthal, 2014).

3.Precautions: It can cause internal bleeding or the external bleeding. Also, the intramuscular injections and trauma must be avoided (Lehne & Rosenthal, 2014). It is significant to avoid the internaljugularandsubclavianvenous punctures (Lehne & Rosenthal, 2014).

Uses: Tissue Plasminogen Activator is used for the patients of stroke, blood clots,Myocardial infarction and other conditions (Lehne & Rosenthal, 2014).