FAROSAR 50

Indications

• Vertigo
• Tinnitus
• Nausea
• Vomiting
• Ménière's disease
• Motion sickness

Dosage

Children: For children aged 5-11 years, the recommended dose is 15 mg taken three times a day. For those aged 12-17 years, the dosage increases to 30 mg three times a day.

Adults: For adults, the typical dosage for the relief of symptoms of vestibular disorders is 30 mg taken three times a day. For motion sickness, 1 tablet (15 mg) should be taken three times a day, ideally starting 1-2 hours before travel.

Mechanism of action

Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Additionally, it binds to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors, contributing to its anti-emetic properties.

Pharmacodynamics

Cinnarizine functions as both an antihistamine and a calcium channel blocker. It acts as a competitive antagonist at histamine H1 receptors, which mediate various physiological activities including smooth muscle contraction and vasodilation. By blocking muscarinic acetylcholine receptors, it also exhibits anti-emetic effects. Its calcium channel blocking capability inhibits stimulation of the vestibular system, reducing symptoms of motion sickness.

Pharmacokinetics

Cinnarizine is well absorbed following oral administration, with peak plasma concentrations typically occurring within 1-3 hours. The drug is extensively metabolized in the liver, and its metabolites are primarily excreted via the kidneys. The half-life of cinnarizine is approximately 4-6 hours, although this may vary based on individual patient factors.

Contra-indications

• Acute porphyrias
• Epilepsy
• Glaucoma (in children)
• Parkinson's disease (in adults)
• Prostatic hypertrophy (in adults)
• Pyloroduodenal obstruction
• Susceptibility to angle-closure glaucoma (in adults)
• Urinary retention

Adverse effects

• Drowsiness
• Dry mouth
• Gastrointestinal disturbances
• Weight gain
• Extrapyramidal symptoms

Interactions

• Sedating antihistamines
• Other CNS depressants

Precautions

• Use with caution in patients with epilepsy
• Use with caution in patients with glaucoma
• Use with caution in patients with prostatic hypertrophy
• Use with caution in patients with Parkinson's disease

Pregnancy

Antihistamines, including Cinnarizine, should be used with caution during pregnancy, particularly in the third trimester, due to potential risks.

Breast-feeding

Cinnarizine is excreted in breast milk; caution is advised when used during breastfeeding.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Cinnarizine 15 mg tablets
• Cinnarizine oral suspension

Indications

• Hypertension
• Chronic heart failure when ACE inhibitors are unsuitable
• Diabetic nephropathy in type 2 diabetes mellitus

Dosage

Children: Refer to the BNF for Children for specific dosing information.

Adults: Initially 50 mg once daily for adults aged 18–75 years, and 25 mg once daily for adults aged 76 years and over. Doses may be increased to 100 mg once daily if necessary.

Mechanism of action

Losartan selectively blocks the binding of angiotensin II to the AT1 receptor, leading to vasodilation, decreased secretion of aldosterone, and reduced blood pressure. This mechanism also contributes to renal protection in diabetic patients by reducing glomerular pressure.

Pharmacodynamics

Losartan exhibits dose-dependent antihypertensive effects, with initial doses often resulting in a reduction of blood pressure within 6 hours. The peak effect is typically reached within 4 to 6 weeks of treatment. Additionally, losartan has a protective effect on renal function in patients with diabetic nephropathy.

Pharmacokinetics

Losartan is well absorbed after oral administration, with a bioavailability of approximately 33%. It is extensively metabolized in the liver to its active metabolite, E3174, which has a longer half-life than losartan itself. The elimination half-life of losartan is around 2 hours, while that of E3174 is approximately 6 to 9 hours. Both losartan and E3174 are primarily excreted in the urine, and renal impairment may affect their clearance.

Contra-indications

• Hypersensitivity to losartan or any of the excipients
• Severe hepatic impairment
• Pregnancy
• Bilateral renal artery stenosis or unilateral renal artery stenosis in a solitary kidney
• History of angioedema

Adverse effects

• Dizziness
• Hypotension
• Hyperkalaemia
• Fatigue
• Postural hypotension
• Abdominal pain
• Nausea
• Diarrhoea
• Headache
• Musculoskeletal pain
• Renal impairment

Interactions

• Other antihypertensive agents may enhance the hypotensive effect
• Potassium supplements or potassium-sparing diuretics may increase the risk of hyperkalaemia
• Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect
• Lithium levels may be increased when taken with losartan

Precautions

• Monitor renal function and electrolytes in patients with renal impairment
• Use with caution in patients with a history of angioedema
• Caution in patients with volume depletion
• Not recommended for use in patients with severe heart failure

Pregnancy

Losartan is contraindicated in pregnancy due to potential harm to the fetus, particularly during the second and third trimesters.

Breast-feeding

It is not known whether losartan is excreted in human milk; caution is advised when administering to breastfeeding women.

Storage

Store at room temperature (15 to 30 degrees Celsius), protected from light and moisture.

Formulations

• Losartan potassium 12.5 mg tablets
• Losartan potassium 25 mg tablets
• Losartan potassium 50 mg tablets
• Losartan potassium 100 mg tablets
• Losartan with hydrochlorothiazide 50 mg/12.5 mg tablets
• Losartan with hydrochlorothiazide 100 mg/12.5 mg tablets

Indications

• Monitoring respiratory function
• Assessment of metabolic status
• Management of respiratory acidosis
• Management of respiratory alkalosis

Dosage

Children: Dosing for interventions related to carbon dioxide levels in pediatric patients should be guided by clinical protocols and the BNF for Children.

Adults: Dosing for interventions related to carbon dioxide levels is typically based on clinical assessment and individual patient needs. Refer to clinical guidelines for specific scenarios.

Mechanism of action

Carbon dioxide acts primarily as a signaling molecule in the body, influencing respiratory drive and blood pH. It is produced during cellular respiration and is a critical component of the bicarbonate buffering system, which helps maintain acid-base homeostasis. Elevated levels of CO2 in the blood stimulate ventilation in the lungs, increasing the rate of gas exchange and facilitating the removal of excess CO2.

Pharmacodynamics

The pharmacodynamic effects of dioxides, particularly carbon dioxide, are closely related to its concentration in the blood. As CO2 levels increase, it leads to respiratory acidosis, which can stimulate the respiratory centers in the brain to increase ventilation. Conversely, low levels of CO2 can cause respiratory alkalosis, potentially leading to decreased respiratory drive. CO2 also plays a role in vasodilation and can affect blood flow and pressure through its influence on smooth muscle tone.

Pharmacokinetics

Carbon dioxide is produced endogenously during metabolic processes and is transported in the bloodstream primarily in three forms: dissolved in plasma, as bicarbonate ions (HCO3-), and bound to hemoglobin. The half-life of CO2 in the bloodstream is very short due to its rapid exchange with alveolar gas in the lungs. The elimination of CO2 occurs through exhalation, making it a dynamic component of respiratory physiology.

Pregnancy

Data on the effects of dioxide during pregnancy are limited. Caution is advised due to potential risks associated with exposure.

Breast-feeding

Limited data are available regarding the excretion of dioxide in human milk. Caution is recommended.

Storage

Store in a cool, dry place, away from direct sunlight and moisture.

Dosage

Children: Refer to the BNF for Children for appropriate dosing information in paediatric cases, especially in instances of overdose.

Adults: Refer to the BNF for specific dosing information based on clinical circumstances, particularly in cases of overdose.

Mechanism of action

Ethylene glycol is metabolized by alcohol dehydrogenase to glycoaldehyde, which is subsequently converted to glycolic, glyoxylic, and oxalic acids. These metabolites contribute to anion gap metabolic acidosis and are responsible for tissue injury through the formation of insoluble calcium oxalate crystals.

Pharmacodynamics

The toxicity of ethylene glycol arises from its metabolites, particularly glycolic and oxalic acids. These compounds induce metabolic acidosis, lead to renal failure through calcium oxalate crystal deposition in the kidneys, and can cause neurological impairment. The anion gap increases due to the accumulation of these acids, leading to complications such as cardiovascular instability and potential multi-organ failure.

Pharmacokinetics

Ethylene glycol is rapidly absorbed after oral ingestion. It undergoes first-pass metabolism primarily in the liver, where it is converted into its toxic metabolites. The elimination half-life of ethylene glycol varies but is generally prolonged in cases of renal impairment. Renal excretion of metabolites contributes to the duration of toxicity, necessitating prompt medical intervention in cases of overdose.

Adverse effects

• Metabolic acidosis
• Renal failure
• CNS depression
• Hypocalcemia
• Cardiovascular collapse
• Pulmonary edema

Precautions

• Use with caution in patients with renal impairment
• Monitor for signs of metabolic acidosis
• Evaluate electrolyte levels, particularly calcium

Pregnancy

There is limited data on the safety of ethylene glycol in pregnancy. It should only be used if clearly needed.

Breast-feeding

It is unknown if ethylene glycol is excreted in human milk. Caution is advised.

Storage

Store in a tightly closed container at room temperature, away from heat and moisture.

Formulations

• Liquid

Indications

• Lactose intolerance
• As a filler or excipient in pharmaceutical formulations

Dosage

Children: Refer to the BNF for Children for specific dosing information based on age and clinical context.

Adults: Refer to the BNF for specific dosing information based on clinical context.

Mechanism of action

Lactose is metabolized in the intestine by the enzyme lactase into its constituent monosaccharides, glucose and galactose. In individuals with lactase deficiency, unabsorbed lactose passes into the colon, where it is fermented by bacteria, leading to gas production and osmotic effects that contribute to diarrhea.

Pharmacodynamics

The pharmacodynamics of lactose are primarily related to its effects on gastrointestinal function. In healthy individuals, lactose is effectively broken down into glucose and galactose, which are absorbed and utilized for energy. In individuals with lactose intolerance, the unabsorbed lactose can cause osmotic diarrhea and colonic fermentation, leading to discomfort and symptoms associated with lactose intolerance.

Pharmacokinetics

Lactose is not absorbed in the gastrointestinal tract until it is hydrolyzed into glucose and galactose by lactase. The absorption of glucose and galactose occurs in the small intestine. The half-life is not applicable as lactose is not typically administered as a medication but is rather ingested as a natural component of food. Its metabolism primarily occurs in the intestine.

Adverse effects

• Bloating
• Diarrhea
• Abdominal pain
• Flatulence

Precautions

• Use with caution in patients with lactose intolerance.
• Consider potential for gastrointestinal upset in sensitive individuals.

Pregnancy

Lactose is generally considered safe for use during pregnancy. However, consult a healthcare professional for individual advice.

Breast-feeding

Lactose is safe to use while breastfeeding, as it is a natural sugar present in breast milk.

Storage

Store in a cool, dry place, away from direct sunlight.

Formulations

• Powder
• Granules
• Tablets
• Syrup

Indications

• Hypertension
• Diabetic nephropathy
• Reduction of stroke risk in certain populations

Dosage

Children: For paediatric patients aged 6 years and older, the starting dose is usually 0.7 mg/kg once daily, with a maximum of 50 mg daily. Dosing should be adjusted based on blood pressure response and tolerance.

Adults: The typical adult dose for hypertension is 50 mg once daily, which may be increased to a maximum of 100 mg once daily, depending on response.

Mechanism of action

Losartan reversibly and competitively prevents angiotensin II from binding to the AT1 receptor in various tissues, including vascular smooth muscle and the adrenal gland. By doing so, it causes relaxation of vascular smooth muscle, leading to decreased blood pressure. Losartan's active metabolite is significantly more potent as an AT1 receptor inhibitor and further enhances the drug's efficacy in blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II.

Pharmacodynamics

Losartan is classified as an angiotensin II receptor blocker that effectively lowers blood pressure and is indicated for diabetic nephropathy. It has a long duration of action, which supports its once-daily administration. Regular monitoring of patients is recommended to assess for hypotension, renal function, and potassium levels, as the drug can affect these parameters.

Pharmacokinetics

Losartan is well absorbed and undergoes extensive first-pass metabolism, resulting in an active metabolite that contributes to its therapeutic effects. The drug is primarily eliminated through the urine and feces. The half-life of losartan and its active metabolite allows for stable plasma concentrations with once-daily dosing, but renal impairment may affect its clearance.

Contra-indications

• Hypersensitivity to losartan or any of its excipients
• Severe hepatic impairment
• Pregnancy

Adverse effects

• Dizziness
• Hypotension
• Hyperkalemia
• Renal impairment
• Fatigue
• Headache
• Diarrhea

Interactions

• Potassium-sparing diuretics may increase the risk of hyperkalemia
• Non-steroidal anti-inflammatory drugs (NSAIDs) may reduce the antihypertensive effect of losartan
• Lithium levels may increase when used concurrently with losartan

Precautions

• Monitor blood pressure regularly
• Assess renal function before and during treatment
• Caution in patients with a history of angioedema
• Use with caution in patients with renal artery stenosis

Pregnancy

Losartan is contraindicated in pregnancy due to potential harm to the fetus.

Breast-feeding

Losartan is excreted in breast milk, caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place at room temperature, away from direct sunlight.

Formulations

• Tablets: 25 mg, 50 mg, 100 mg

Indications

• Constipation
• Bowel preparation prior to surgical procedures or diagnostic tests

Dosage

Children: Refer to specific guidelines or BNF for Children for dosing information.

Adults: Refer to specific guidelines or BNF for detailed dosing information.

Mechanism of action

Polyethylene glycol works by osmotically retaining water in the intestinal lumen, which increases the water content of the stool. This enhances the passage of stool through the intestines and promotes bowel movements. The high molecular weight of polyethylene glycol prevents its absorption in the gastrointestinal tract, ensuring that it remains in the lumen to exert its effects.

Pharmacodynamics

The pharmacodynamic profile of polyethylene glycol involves its ability to increase stool water content, thereby reducing stool consistency and facilitating easier passage. It does not stimulate intestinal motility directly but rather relies on the osmotic effect to promote bowel evacuation. The onset of action typically occurs within 24 to 96 hours after ingestion.

Pharmacokinetics

Polyethylene glycol is not absorbed systemically, and its pharmacokinetics are characterized by its presence solely in the gastrointestinal tract. It is excreted unchanged in the stool. The volume of polyethylene glycol administered can influence the effectiveness and timing of its action, but its absorption is negligible, making systemic side effects rare.

Adverse effects

• Abdominal cramping
• Diarrhea
• Nausea
• Vomiting
• Bloating
• Flatulence

Precautions

• Use with caution in patients with gastrointestinal disorders or bowel obstruction.
• Ensure adequate hydration during use to prevent dehydration.

Pregnancy

Polyethylene glycol is generally considered safe during pregnancy, but should be used under medical supervision.

Breast-feeding

Polyethylene glycol is excreted in breast milk in very small amounts and is generally regarded as safe during breastfeeding.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Powder for oral solution
• Liquid formulation

Dosage

Children: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Adults: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Mechanism of action

The mechanism of action for purified compounds varies widely depending on the specific substance. Generally, purified drugs exert their effects by interacting with specific biological targets, such as receptors, enzymes, or ion channels, leading to a desired therapeutic effect. This interaction can involve binding to receptors to activate or inhibit signaling pathways, modulating enzymatic activity, or altering physiological processes.

Pharmacodynamics

Pharmacodynamics describes the effects of a drug on the body and the relationship between drug concentration and effect. For purified drugs, this can involve dose-response relationships and the time course of their action. The purified form often enhances potency and reduces variability in response among patients, which can lead to more predictable therapeutic outcomes. The overall effect is determined by the drug's affinity for its target, the efficacy of the drug-receptor interaction, and the downstream signaling pathways activated as a result of this interaction.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of a drug. For purified substances, absorption can be more efficient due to the absence of impurities that may affect solubility or stability. Distribution may also be enhanced, leading to higher bioavailability. Metabolism can be influenced by the structure of the purified compound, as it may be metabolized more readily by liver enzymes. Excretion typically occurs through the kidneys or liver, depending on the molecular characteristics of the purified drug.

Pregnancy

Consult with a healthcare professional, as the safety of purified forms of medications during pregnancy may vary depending on the specific substance.

Breast-feeding

Consult with a healthcare professional, as the safety of purified forms of medications during breastfeeding may vary depending on the specific substance.

Storage

Store in a cool, dry place, away from light and moisture, and keep out of reach of children.

Indications

• Orthopedic implants
• Dental implants
• Prosthetic devices
• Surgical instruments

Mechanism of action

Titanium does not have a specific mechanism of action as it is not a drug in the traditional sense. Instead, its biocompatibility allows it to integrate with biological tissues without eliciting significant immune responses, making it suitable for use in implants and prosthetic devices. The presence of titanium ions can influence biological processes, including cell proliferation and differentiation.

Pharmacodynamics

Titanium itself does not exhibit pharmacodynamics as it is not administered as a drug. Its interactions within biological systems are primarily mechanical and structural, providing support and stability in orthopedic and dental applications. The biocompatibility of titanium allows for favorable tissue integration and reduced rejection rates compared to other materials.

Pharmacokinetics

As titanium is not a pharmacological agent, traditional pharmacokinetic parameters such as absorption, distribution, metabolism, and excretion do not apply. Titanium is typically utilized in solid forms, such as implants, where it remains localized and does not undergo metabolism or systemic circulation.

Pregnancy

There is limited data on the use of titanium during pregnancy. Consult a healthcare professional before use.

Breast-feeding

There is limited data on the excretion of titanium in breast milk. Consult a healthcare professional before use.

Storage

Store in a cool, dry place away from direct sunlight.

Mechanism of action

Cinnarizine inhibits contractions of vascular smooth muscle cells by blocking L-type and T-type voltage gated calcium channels. Cinnarizine has also been implicated in binding to dopamine D2 receptors, histamine H1 receptors, and muscarinic acetylcholine receptors.

Pharmacodynamics

Cinnarizine is an antihistamine and a calcium channel blocker. Histamines mediate a number of activities such as contraction of smooth muscle of the airways and gastrointestinal tract, vasodilatation, cardiac stimulation, secretion of gastric acid, promotion of interleukin release and chemotaxis of eosinophils and mast cells. Competitive antagonists at histamine H1 receptors may be divided into first (sedating) and second (non-sedating) generation agents. Some, such as Cinnarizine also block muscarinic acetylcholine receptors and are used as anti-emetic agents. Cinnarizine through its calcium channel blocking ability also inhibits stimulation of the vestibular system.

Mechanism of action

Ethylene glycol is metabolized by alcohol dehydrogenase to glycoaldehyde, which is then metabolized to glycolic, glyoxylic, and oxalic acids. These acids, along with excess lactic acid are responsible for the anion gap metabolic acidosis. Oxalic acid readily precipitates with calcium to form insoluble calcium oxalate crystals. Tissue injury is caused by widespread deposition of oxalate crystals and the toxic effects of glycolic and glyoxylic acids.

Mechanism of action

Losartan reversibly and competitively prevents angiotensin II binding to the AT₁ receptor in tissues like vascular smooth muscle and the adrenal gland. Losartan and its active metabolite bind the AT₁ receptor with 1000 times more affinity than they bind to the AT₂ receptor. The active metabolite of losartan is 10-40 times more potent by weight than unmetabolized losartan as an inhibitor of AT₁ and is a non-competitive inhibitor. Losartan's prevention of angiotensin II binding causes vascular smooth muscle relaxation, lowering blood pressure. Angiotensin II would otherwise bind to the AT₁ receptor and induce vasoconstriction, raising blood pressure. Angiotensin II (formed from angiotensin I in a reaction catalyzed by angiotensin converting enzyme (ACE, kininase II)), is a potent vasoconstrictor, the primary vasoactive hormone of the renin-angiotensin system and an important component in the pathophysiology of hypertension. It also stimulates aldosterone secretion by the adrenal cortex. Losartan and its principal active metabolite block the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor found in many tissues, (e.g., vascular smooth muscle, adrenal gland). There is also an AT2 receptor found in many tissues but it is not known to be associated with cardiovascular homeostasis. Both losartan and its principal active metabolite do not exhibit any partial agonist activity at the AT1 receptor and have much greater affinity (about 1000-fold) for the AT1 receptor than for the AT2 receptor. In vitro binding studies indicate that losartan is a reversible, competitive inhibitor of the AT1 receptor. The active metabolite is 10 to 40 times more potent by weight than losartan and appears to be a reversible, non-competitive inhibitor of the AT1 receptor. Neither losartan nor its active metabolite inhibits ACE (kininase II, the enzyme that converts angiotensin I to angiotensin II and degrades bradykinin); nor do they bind to or block other hormone receptors or ion channels known to be important in cardiovascular regulation. We investigated the effects of angiotensin II (Ang II) type 1 receptor blockade with losartan on the renin-angiotensin-aldosterone system in hypertensive patients (supine diastolic blood pressure, 95 to 110 mm Hg). Qualifying patients (n = 51) were allocated to placebo, 25 or 100 mg losartan, or 20 mg enalapril. Blood pressure, plasma drug concentrations, and renin-angiotensin-aldosterone system mediators were measured on 4 inpatient days: end of placebo run-in, after first dose, and 2 and 6 weeks of treatment. Plasma drug concentrations were similar after the first and last doses of losartan. At 6 weeks, 100 mg losartan and 20 mg enalapril showed comparable antihypertensive activity. Four hours after dosing, compared with the run-in day, 100 mg losartan increased plasma renin activity 1.7-fold and Ang II 2.5-fold, whereas enalapril increased plasma renin activity 2.8-fold and decreased Ang II 77%. Both drugs decreased plasma aldosterone concentration. For losartan, plasma renin activity and Ang II increases were greater at 2 than at 6 weeks. Effects of losartan were dose related. After the last dose of losartan, plasma renin activity and Ang II changes were similar to placebo changes by 36 hours. These results indicate that long-term blockade of the feedback Ang II receptor in hypertensive patients produces modest increases of plasma renin activity and Ang II that do not appear to affect the antihypertensive response to the antagonist. /Salt not specified/ IL-1beta is a potent proinflammatory, pro-fibrogenetic and pro-athrosclerosis cytokine which has been shown to play an important role in an expanding number of noninfectious, chronic inflammatory conditions including cardiovascular disease, renal fibrosis, rheumatoid arthritis and even type 2 diabetes. Losartan is an angiot

Pharmacodynamics

Losartan is an angiotensin II receptor blocker used to treat hypertension, diabetic nephropathy, and to reduce the risk of stroke. Losartan has a long duration of action as it is given once daily. Patients taking losartan should be regularly monitored for hypotension, renal function, and potassium levels.