Drug Literature Scrapbook

PHARMACOLOGY
S.Y. 2024-2025

Submitted To : Mr. Ronald Allan C. Librando, RN

Submitted By: Vernaly A. Guanzon, BSN-II

1. FELODIPINE - PENDIL
 Dosages
Dosage Forms and Strengths
Tablets, extended-release

 2.5 mg
 5 mg
 10 mg

Indication

For the treatment of mild to moderate essential hypertension.

Pharmacodynamics

Felodipine belongs to the dihydropyridine (DHP) class of calcium channel

blockers (CCBs), the most widely used class of CCBs. There are at least five

different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type.

It was widely accepted that CCBs target L-type calcium channels, the major

channel in muscle cells that mediates contraction; however, some studies have

shown that felodipine also binds to and inhibits T-type calcium channels.

Mechanism of action

Felodipine decreases arterial smooth muscle contractility and subsequent

vasoconstriction by inhibiting the influx of calcium ions through voltage-gated L-

type calcium channels. It reversibly competes against nitrendipine and other DHP

CCBs for DHP binding sites in vascular smooth muscle and cultured rabbit atrial

cells.

Absorption

Is completely absorbed from the gastrointestinal tract; however, extensive first-

pass metabolism through the portal circulation results in a low systemic

availability of 15%. Bioavailability is unaffected by food.

Volume of distribution
  10 L/kg

Metabolism

Hepatic metabolism primarily via cytochrome P450 3A4. Six metabolites with no

appreciable vasodilatory effects have been identified.

Contraindications

Felodipine in contraindicated in those known to be hypersensitive to it or to

other calcium channel antagonists.

Adverse Effects

Adverse effects associated with the use of felodipine include dizziness,

flushing, gingival hyperplasia, headache, and edema. Included among more

serious side effects associated with felodipine are myocardial infarction,

angina, tachycardia, and hypotension.

2. GLIMEPERIDE – Amaryl

Dosages

 1 mg oral tablets

 2 mg oral tablets

 3 mg oral tablets
  4 mg oral tablets

 6 mg oral tablets

 8 mg oral tablets

Indication

Glimepiride is indicated for the management of type 2 diabetes in adults as an adjunct

to diet and exercise to improve glycemic control as monotherapy.It may also be

indicated for use in combination with metformin or insulin to lower blood glucose in

patients with type 2 diabetes whose high blood sugar levels cannot be controlled by diet

and exercise in conjunction with an oral hypoglycemic (a drug used to lower blood sugar

levels) agent alone.

Pharmacodynamics

Glimepiride stimulates the secretion of insulin granules from the pancreatic beta cells

and improves the sensitivity of peripheral tissues to insulin to increase peripheral

glucose uptake, thus reducing plasma blood glucose levels and glycated hemoglobin

(HbA1C) levels. A multi-center, randomized, placebo-controlled clinical trial evaluated

the efficacy of glimepiride (1–8 mg) as monotherapy titrated over 10 weeks compared

with placebo in T2DM subjects who were not controlled by diet alone.

Mechanism of action

ATP-sensitive potassium channels on pancreatic beta cells that are gated by intracellular

ATP and ADP. The hetero-octomeric complex of the channel is composed of four pore-

forming Kir6.2 subunits and four regulatory sulfonylurea receptor (SUR) subunits.

Alternative splicing allows the formation of channels composed of varying subunit

isoforms expressed at different concentrations in different tissues.

Absorption
 Glimepiride is completely absorbed after oral administration within 1 hour of

administration with a linear pharmacokinetics profile.1 Following administration of a

single oral dose of glimepiride in healthy subjects and with multiple oral doses with type

2 diabetes, the peak plasma concentrations (Cmax) were reached after 2 to 3 hours

post-dose.

Volume of distribution

Following intravenous dosing in healthy subjects, the volume of distribution was

8.8 L (113 mL/kg).8

Metabolism

Glimepiride is reported to undergo hepatic metabolism. Following either an intravenous

or oral dose, glimepiride undergoes oxidative biotransformation mediated by CYP2C9

enzyme to form a major metabolite, cyclohexyl hydroxymethyl derivative (M1), that is

pharmacologically active. M1 can be further metabolized to the inactive metabolite

carboxyl derivative (M2) by one or several cytosolic enzymes.

Adverse Effects

 Allergic reactions—skin rash, itching, hives, swelling of the face, lips, tongue, or

throat

 Low blood sugar (hypoglycemia)—tremors or shaking, anxiety, sweating, cold or

clammy skin, confusion, dizziness, rapid heartbeat

Contraindications

 Hypersensitivity; sulfa allergy

 Type 1 diabetes

 Diabetic ketoacidosis (with or without coma)

 Complicated gestational diabetes mellitus

 3. LANSOPRAZOLE - Prevacid

Dosages

 15 mg delayed-release oral capsules

 30 mg delayed-release oral capsules

 15 mg delayed-release orally disintegrating tablets

 30 mg delayed-release orally disintegrating tablets

Indication

Lansoprazole is used to reduce gastric acid secretion and is approved for short term

treatment of active gastric ulcers, active duodenal ulcers, erosive reflux oesophagitis,

symptomatic gastroesophageal reflux disease, and non-steroidal anti-inflammatory drug

(NSAID) induced gastric and duodenal ulcers.

Pharmacodynamics

Lansoprazole decreases gastric acid secretion by targeting H+,K+-ATPase, which is the

enzyme that catalyzes the final step in the acid secretion pathway in parietal

cells. 6 Conveniently, lansoprazole administered any time of day is able to inhibit both

daytime and nocturnal acid secretion.6 The result is that lansoprazole is effective at

healing duodenal ulcers, reduces ulcer-related pain, and offers relief from symptoms of

heartburn.

Mechanism of action

As a PPI, lansoprazole is a prodrug and requires protonation via an acidic environment

to become activated. 3 Once protonated, lansoprazole is able to react with cysteine

residues, specifically Cys813 and Cys321, on parietal H+,K+-ATPase resulting in stable

 disulfides.35 PPI's in general are able to provide prolonged inhibition of acid secretion

due to their ability to bind covalently to their targets.

Absorption

The oral bioavailability of lansoprazole is reported to be 80-90%2 and the peak plasma

concentration(Cmax) is achieved about 1.7 hours after oral dosing.Label Food reduces the

absorption of lansoprazole (both Cmax and AUC are reduced by 50-70%); therefore,

patients should be instructed to take lansoprazole before meals.

Volume of distribution

The apparent volume of distribution of lansoprazole is 0.4 L/kg.

Metabolism

Lansoprazole is predominantly metabolized in the liver by CYP3A4 and

CYP2C19. 3 The resulting major metabolites are 5-hydroxy lansoprazole and the

sulfone derivative of lansoprazole.

Adverse Effects

 diarrhea

 stomach pain

 nausea

 headache

 constipation

Contraindications

 Hypersensitivity to lansoprazole or other proton pump inhibitors

4. MONTELUKAST SODIUM - Singulair

Dosages

 4 mg chewable tablets

 5 mg chewable tablets

 4 mg oral granules

 10 mg oral tablets

INDICATION

Montelukast is used to prevent wheezing, difficulty breathing, chest tightness, and coughing

caused by asthma in adults and children 12 months of age and older. Montelukast is also used

to prevent bronchospasm (breathing difficulties) during exercise in adults and children 6 years of

age and older. Montelukast is also used to treat the symptoms of seasonal (occurs only at

certain times of the year), allergic rhinitis (a condition associated with sneezing and stuffy, runny

or itchy nose) in adults and children 2 years of age and older, and perennial (occurs all year

round) allergic rhinitis in adults and children 6 months of age and older.

Pharmacodynamics

Montelukast is a leukotriene receptor antagonist that demonstrates a marked affinity and

selectivity to the cysteinyl leukotriene receptor type-1 in preference to many other crucial

airway receptors like the prostanoid, cholinergic, or beta-adrenergic receptors.3,4,5,6,7,8,9 As

a consequence, the agent can elicit substantial blockage of LTD4 leukotriene-mediated

bronchoconstriction with doses as low as 5 mg.3,4,5,6,7,8,9 Moreover, a placebo-controlled,

crossover study (n=12) demonstrated that montelukast is capable of inhibiting early and

late phase bronchoconstriction caused by antigen challenge by 75% and 57%

respectively.

Mechanism of action

Cysteinyl leukotrienes (CysLT) like LTC4, LTD4, and LTE4, among others, are

eicosanoids released by a variety of cells like mast cells and eosinophils.3,4,5,6,7,8,9 When
 such CysLT bind to corresponding CysLT receptors like CysLT type-1 receptors located

on respiratory airway smooth muscle cells, airway macrophages, and on various pro-

inflammatory cells like eosinophils and some specific myeloid stem cells activities that

facilitate the pathophysiology of asthma and allergic rhinitis are stimulated.

Absorption

It has been observed that montelukast is quickly absorbed following administration by

the oral route.3,4,5,6,7,8,9 The oral bioavailability documented for the drug is

64%.3,4,5,6,7,8,9 Furthermore, it seems that having a regular meal in the morning or even a

high fat snack in the evening does not affect the absorption of montelukast.

Volume of distribution

The steady-state volume of distribution recorded for montelukast is an average between

8 to 11 litres.

Metabolism

It has been determined that montelukast is highly metabolized and typically so by the

cytochrome P450 3A4, 2C8, and 2C9 isoenzymes.3,4,5,6,7,8,9 In particular, it seems that the

CYP2C8 enzymes play a significant role in the metabolism of the

drug.3,4,5,6,7,8,9 Nevertheless, at therapeutic doses, the plasma concentrations of

montelukast metabolites are undetectable at steady state in adults and pediatric

patients.

Adverse Effects

 stomach pain, diarrhea;

 fever or other flu symptoms;

 ear pain or full feeling, trouble hearing;

 headache; or

 cold symptoms such as runny or stuffy nose, sinus pain, cough, sore throat.

CONTRAINDICATIONS

Hypersensitivity to any component of this product.