FORTIDE INHALER( Budedsoride/Formoterol fumerate dehydrate 2000mcg / 6mcg)

Indications

• Chronic asthma
• Chronic obstructive pulmonary disease (COPD)
• Reversible airways obstruction
• Prophylaxis of exercise-induced bronchospasm

Dosage

Children: Child 6–11 years: 12 micrograms twice daily (maximum daily dose 24 micrograms). Child 12–17 years: 12 micrograms twice daily, may

Adults: 6–12 micrograms by inhalation 1–2 times a day, increased if necessary up to 24 micrograms twice daily (max. per dose 36 micrograms), with a maximum daily dose of 48 micrograms.

Mechanism of action

Formoterol fumarate acts as an agonist at beta-2 adrenergic receptors located on bronchial smooth muscle. Upon binding, it activates adenylate cyclase, increasing intracellular cyclic AMP (cAMP) levels, leading to relaxation of bronchial smooth muscle and bronchodilation. This mechanism results in improved airflow and reduced resistance in the airways.

Pharmacodynamics

The pharmacodynamic effect of formoterol fumarate includes bronchodilation and relief of bronchospasm associated with asthma and COPD. The duration of action is approximately 12 hours, allowing for twice-daily dosing in many cases. Formoterol also exhibits some anti-inflammatory effects, although its primary role is as a bronchodilator.

Pharmacokinetics

Formoterol fumarate is well-absorbed following inhalation, with peak plasma concentrations typically occurring within 15 to 30 minutes. It undergoes extensive metabolism in the liver, primarily via the cytochrome P450 system. The elimination half-life is approximately 10 hours. Renal impairment may necessitate dose adjustments, especially in severe cases, while hepatic impairment is advised against due to the risk of unpredictable conversion to terbutaline.

Contra-indications

• Hypersensitivity to formoterol or any component of the formulation
• Severe impairment or cirrhosis of liver
• Rapidly deteriorating asthma

Adverse effects

• Anxiety
• Abnormal behaviour
• Muscle cramps
• Sleep disorders
• Akathisia
• Angioedema
• Bronchospasm
• Circulatory collapse
• Dizziness
• Hypokalaemia
• Hypotension
• Myocardial ischaemia
• Nausea
• Skin reactions

Interactions

• Concomitant use with theophylline and its derivatives may potentiate hypokalaemia
• Corticosteroids may also increase the risk of hypokalaemia
• Diuretics can lead to additive effects on serum potassium levels

Precautions

• Caution in patients with a history of cardiovascular disease
• Monitor potassium levels in patients on high doses
• Use with caution in patients with severe asthma or those requiring high doses of beta-agonists

Pregnancy

Manufacturer advises to avoid use due to lack of information on safety during pregnancy.

Breast-feeding

Manufacturer advises to avoid use due to lack of information on safety during breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Inhalation powder (various dosage forms including 6 micrograms, 12 micrograms, and 24 micrograms per dose)

Indications

• Asthma
• Chronic obstructive pulmonary disease (COPD)
• Ulcerative colitis
• Crohn's disease

Dosage

Children: Refer to the BNF for Children for specific dosing information based on the child's age and condition.

Adults: Refer to specific guidelines for dosing based on the condition being treated, typically starting with the lowest effective dose.

Mechanism of action

Budesonide exerts its effects by binding to glucocorticoid receptors in target tissues, leading to the modulation of gene expression. This interaction inhibits the production of pro-inflammatory cytokines and chemokines, thereby reducing inflammation and enhancing the resolution of the inflammatory response. Additionally, budenoside inhibits the activation of inflammatory cells, including eosinophils and macrophages.

Pharmacodynamics

Budesonide has potent anti-inflammatory effects, which help to alleviate symptoms associated with asthma and other inflammatory conditions. Its local action in the lungs and intestines allows for effective control of inflammation with fewer systemic effects compared to other corticosteroids. The onset of action can vary, but symptom relief typically occurs within hours after administration.

Pharmacokinetics

Budesonide is administered via inhalation or rectal routes, leading to a significant first-pass metabolism in the liver. This results in lower bioavailability compared to systemic corticosteroids. The half-life of budenoside is approximately 2 to 3 hours, with a peak plasma concentration occurring within 1 to 2 hours after inhalation. The drug is primarily eliminated through hepatic metabolism, and its metabolites are excreted in urine.

Adverse effects

• Cough
• Oral thrush
• Hoarseness
• Pneumonia
• Adrenal suppression
• Increased risk of infections

Interactions

• CYP3A4 inhibitors may increase budesonide levels
• CYP3A4 inducers may decrease budesonide levels

Precautions

• Monitor for signs of adrenal suppression
• Use with caution in patients with a history of tuberculosis or fungal infections
• Assess for potential drug interactions

Pregnancy

Budesonide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is categorized as pregnancy category B.

Breast-feeding

Budesonide can be excreted in breast milk, but the amounts are considered to be low. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat. Keep the inhaler in an upright position.

Formulations

• Inhalation aerosol
• Inhalation powder
• Oral capsules
• Nasal spray

Indications

• Mild to moderate dehydration
• Severe dehydration
• Diarrhea-related dehydration
• Vomiting-related dehydration
• Heat-related illnesses
• Post-operative fluid replacement

Dosage

Children: In children, the oral rehydration solution is typically administered at a rate of 75

Adults: The specific dosage for rehydration will vary based on the severity of dehydration. In mild cases, oral rehydration solutions can be administered at a rate of 50-100 mL/kg over 2-4 hours. For moderate to severe dehydration, intravenous fluids may be indicated, and specific protocols should be followed based on clinical guidelines.

Mechanism of action

Dehydration itself does not have a mechanism of action as it is a physiological state rather than a pharmacological agent. However, the treatment for dehydration typically involves the administration of fluids and electrolytes, either orally or intravenously, to restore hydration status. The rehydration process helps to restore normal blood volume and electrolyte balance, facilitating cellular functions and overall metabolic processes.

Pharmacodynamics

The pharmacodynamics of rehydration solutions involve the restoration of body fluid levels and the correction of electrolyte imbalances. Oral rehydration solutions (ORS) contain a balanced ratio of salts and sugars, which enhance the absorption of water in the intestines. This process helps to re-establish osmotic balance, improve hydration, and support physiological functions. In severe cases, intravenous fluids may be required to rapidly replenish lost fluids and electrolytes.

Pharmacokinetics

The pharmacokinetics of rehydration fluids depend on the type of fluid administered. Oral rehydration solutions are absorbed primarily in the small intestine, with the absorption rate influenced by the osmolarity and composition of the solution. Intravenous fluids are distributed directly into the bloodstream, with effects seen almost immediately. The elimination of excess fluids occurs through renal excretion, which helps maintain homeostasis.

Contra-indications

• Hypersensitivity to the active substance or any of the excipients
• Severe dehydration
• Acute kidney injury

Adverse effects

• Electrolyte imbalance
• Hypotension
• Dizziness
• Dry mouth
• Thirst
• Skin rash
• Nausea
• Vomiting

Interactions

• Caution with concomitant use of diuretics
• May interact with other medications affecting electrolyte levels
• Potential interaction with medications that affect kidney function

Precautions

• Use with caution in patients with renal impairment
• Monitor electrolyte levels during therapy
• Ensure adequate hydration during treatment

Pregnancy

Use only if clearly needed and prescribed by a healthcare professional. Risk-benefit should be considered.

Breast-feeding

Consult healthcare provider before use. Monitor infant for any adverse effects.

Storage

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

Formulations

• Oral solution
• Oral powder
• Intravenous solution

Indications

• Asthma
• Chronic obstructive pulmonary disease (COPD)

Dosage

Children: Refer to BNF for Children for specific dosing recommendations based on age and weight.

Adults: Refer to BNF for specific dosing guidance, typically involving the use of metered-dose inhalers or nebulizers.

Mechanism of action

Formoterol selectively binds to and activates beta2-adrenergic receptors, predominantly located in bronchial smooth muscle. This activation stimulates adenylyl cyclase, leading to increased levels of cyclic AMP (cAMP). Elevated cAMP causes relaxation of bronchial smooth muscle and dilation of the airways. Additionally, formoterol inhibits the release of hypersensitivity mediators, such as histamine and leukotrienes, from mast cells, further contributing to its bronchodilator effect.

Pharmacodynamics

As a bronchodilator, formoterol works locally in the lungs to relax smooth muscle and open the airways. It provides both a rapid onset of action and a prolonged duration, making it suitable for the management of chronic respiratory conditions. However, it should not be used as monotherapy in asthma management due to an associated increased risk of asthma-related death when not combined with inhaled corticosteroids.

Pharmacokinetics

Formoterol is administered via inhalation, allowing for direct delivery to the lungs. It has a rapid onset of action, typically within 2-3 minutes, and is characterized by a long duration of action, up to 12 hours. The pharmacokinetics of formoterol may vary based on individual patient factors, including age, lung function, and concurrent medications.

Contra-indications

• Hypersensitivity to formoterol or any of its components
• Severe uncontrolled asthma
• Acute bronchospasm
• Cardiovascular disorders
• Use of monoamine oxidase inhibitors (MAOIs) within 14 days

Adverse effects

• Tachycardia
• Palpitations
• Tremor
• Headache
• Nervousness
• Dizziness
• Nausea
• Muscle cramps
• Hypokalemia
• Hyperglycemia

Interactions

• Other sympathomimetics
• Beta-blockers (may reduce effectiveness of formoterol)
• Diuretics (may increase the risk of hypokalemia)
• Monoamine oxidase inhibitors (MAOIs)
• Tricyclic antidepressants

Precautions

• Caution in patients with cardiovascular disorders
• Caution in patients with diabetes mellitus
• Use with caution in patients with hyperthyroidism
• Monitor for worsening of asthma symptoms
• Avoid use as a rescue medication

Pregnancy

Formoterol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult a healthcare provider.

Breast-feeding

It is not known whether formoterol is excreted in human milk. Caution should be exercised when prescribing to nursing women.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Formulations

• Aerosol inhaler
• Dry powder inhaler
• Nebuliser solution

Dosage

Children: Refer to official dosing guidelines for paediatric indications and dosages.

Adults: Refer to official dosing guidelines for specific indications and dosages.

Mechanism of action

Fumarate acts primarily as an intermediate in the TCA cycle, where it is converted to malate by the enzyme fumarase. This process is essential for the continuation of aerobic respiration, facilitating the conversion of carbohydrates, fats, and proteins into energy. Additionally, fumarate can participate in redox reactions, influencing cellular metabolism and signaling pathways.

Pharmacodynamics

Fumarate influences various metabolic pathways, including the urea cycle and glycolysis, by participating in electron transfer processes. Its role in the TCA cycle is vital for ATP production, and its interaction with other metabolic pathways helps regulate energy homeostasis and the balance of nitrogen in the body.

Pharmacokinetics

The pharmacokinetics of fumarate involve its absorption, distribution, metabolism, and excretion. Fumarate is readily absorbed when introduced into the body and is distributed to various tissues where it participates in metabolic processes. The metabolic conversion of fumarate occurs primarily in the mitochondria through the TCA cycle, and its elimination from the body is facilitated by renal pathways.

Pregnancy

There are no established guidelines regarding the use of fumerate during pregnancy. Consult healthcare professionals for individual risk assessment.

Breast-feeding

The safety of fumerate during breastfeeding has not been established. Caution is advised and consultation with healthcare professionals is recommended.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Mechanism of action

Formoterol is a relatively selective long-acting agonist of beta₂-adrenergic receptors, although it does carry some degree of activity at beta₁ and beta₃ receptors. Beta₂ receptors are found predominantly in bronchial smooth muscle (with a relatively minor amount found in cardiac tissue) whereas beta₁ receptors are the predominant adrenergic receptors found in the heart - for this reason, selectivity for beta₂ receptors is desirable in the treatment of pulmonary diseases such as COPD and asthma. Formoterol has demonstrated an approximately 200-fold greater activity at beta₂ receptors over beta₁ receptors. On a molecular level, activation of beta receptors by agonists like formoterol stimulates intracellular adenylyl cyclase, an enzyme responsible for the conversion of ATP to cyclic AMP (cAMP). The increased levels of cAMP in bronchial smooth muscle tissue result in relaxation of these muscles and subsequent dilation of the airways, as well as inhibition of the release of hypersensitivity mediators (e.g. histamine, leukotrienes) from culprit cells, especially mast cells. Formoterol is a long-acting selective stimulator of the beta2-adrenergic receptors in bronchial smooth muscle. This stimulation causes relaxation of smooth muscle fibers and produces bronchodilation. Formoterol stimulates beta2-adrenergic receptors and apparently has little or no effect on beta1- or alpha-adrenergic receptors. The drug's beta-adrenergic effects appear to result from stimulation of the production of cyclic adeno-3'-5'-monophosphate (cAMP)by activation of adenyl cyclase. Cyclic AMP mediate numerous cellular responses, increased concentrations of cAMP are associated with relaxation of bronchial smooth muscle and suppression of some aspects of inflammation, such as inhibition of release proinflammatory mast cell mediators(eg histamine, leukotrienes).

Pharmacodynamics

Formoterol works locally in the lungs as a bronchodilator, relaxing smooth muscle and opening up the airways. It possesses both a rapid onset of action (approximately 2-3 minutes) and a long duration of action (up to 12 hours). The use of long-acting beta-agonists (LABAs), such as formoterol, without concomitant inhaled corticosteroids in asthmatic patients should be avoided, as LABA monotherapy has been associated with an increased risk of asthma-related death.