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Decongestants, anti histamines, antitussive.pptx
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- 2. Decongestants are medicationsthat relieve nasal congestion by narrowing the blood vessels in the nasal passages, reducing swelling and congestion. Indication and uses • INDICATIONS • Allergic rhinitis • Allergies • Sinusitis • Eustashian tube dysfuction • Upper respiratory congestion CONTRAINDICATION • Glucoma • uncontrolled BP • Heart conditions • Thyroid problems • Enlarged prostate • Diabetes
- 3. Oral Decongestants Sympathomimitic Agents •Ephedrine, Pseudoephedrine, Phenylephrine (less commonly used). • Mechanism of Action: • Oral Decongestants: Pseudoephedrine is a sympathomimetic amine and works by stimulating alpha-adrenergic receptors on blood vessels in the nasal mucosa. This stimulation causes vasoconstriction, reducing blood flow to the nasal passages and relieving congestion. • Oral Decongestants: • Pseudoephedrine: The typical adult dose is 60 mg to 120 mg every 4 to 6 hours, with a maximum daily dose of 240 mg. Pseudoephedrine is available as oral tablets or capsules. • Phenylephrine: The typical adult dose is 10 mg every 4 hours, with a maximum daily dose of 60 mg. Phenylephrine is less commonly used due to its shorter duration of action compared to pseudoephedrine. It is available as oral tablets or capsules.
- 4. Topical Nasal Decongestants Sympathomimiticagents • Oxymetazoline and Xylometazoline are also sympathomimetic agents that act by constricting blood vessels in the nasal mucosa when applied topically. This action reduces blood flow and swelling, providing relief from nasal congestion. • Doses and Routes of Administration: • Topical Nasal Decongestants (Nasal Sprays/Drops): • Oxymetazoline: The usual dose is one to two sprays (0.05% strength) in each nostril every 10 to 12 hours. Do not use for more than 3 to 5 days consecutively to avoid rebound congestion. Oxymetazoline is available as nasal sprays. • Xylometazoline: The usual dose is one to two drops (0.1% strength) in each nostril every 8 to 10 hours. Do not use for more than 3 to 5 days consecutively to avoid rebound congestion. Xylometazoline is available as nasal drops. • Phenylphrine • Epinephrine • CORTICOSTEROIDS • SALINE
- 5. Side Effects • IncresedHeart rate • Increased BP • Nervousness or restlessness • Insomnia • Dry mouth and throat • N&V, Headache • Rebound Congestion
- 6. Expectorants and Antitussives •Expectorants are drugs that are increase bronchial secretion or reduce its viscosity, facilitating its removal by coughing and enhance the clearance of mucus.”. Also called as Mucokinetics.
- 7. Classification • Sodium orPotassium citrate, Potassium iodide,( Not Used) Guaiphenesin- 200-400mg qd • Ivy Leaf extract(herbal) • MOA— not fully understood –increases the volume and fluidity of resp. Secretions—effective when taken adequate amount off water—hydration • A. Bronchial Secretion Enhancers
- 8. B. Mucolytics • Ambroxolhydrochloride-tab. 30mg , 15mg/5ml • Acetylecysteine 10%-20% Solution nebuliztaion, 200mg/sachet PO • Carbocysteine tab. 375mg tid, 250mg/5ml syrup • Bromhexine (Not Used) • Mechanism of action • Ambroxol—increases the production and secretion of surfactant –breaks down acid mucopolysachride fibre of mucus— helps in reduce surface tension of mucus— less sticky — easier to expel through coughing • Acetyle Cystein—break disulphide bonds of mucus—reduces viscosity • These drugs also act as antioxidants— has Anti-inflammatory action
- 9. Antitussives • These aredrugs that act in the CNS to raise the threshold of cough centre or act peripherally in the respiratory tract to reduce tussal impulses, or both these actions.
- 10. Classification of Antitussives Pharmacokinetics • 1. Opioid Derivaties • Codeine 5-10mg/5ml • Ethymorphine 100-200mg/5ml Pholcodein 2.5-5ml/5ml • Well absorbed • Metabolism-cypp2d6 into active metabolite morphine, hydromorphone • Bioavailability -50% • Elimination urine Mechanism of action • Acting centrally—Mu opioid recptor medullary cough centre— also have peripheral action on cough receptors.— decreases cough reflexes • Side effects — sedation, constipation, addiction
- 11. 2. Non-opioid antitussives Pharmacokinetics •Dextromethorphan 5-20mg/5ml • Chlophedianol(clofedanol) 5–12mg/5ml • Noscopine 1.3-15mg/5ml • Rapidly absorbed • Liver enzymes • Half life— 2-4 hrs. And 1-4 hrs for nascopine • Bioavailability 30%- • Elimination throgh bile and urine Pharmacodynamics • Nascopine depresses cough by its delta- opioid receptor agonist • Dextrometharphan- NMDA, glutamate and Sigma 1 in the brain— thoughtto Supression cough reflexes • Clofedanol binds to sigma 1 receptor in the brain – anaesthetic, antispasmodic and antihistamine effects, • SIDE EFFECTS • Dizziness, hallucination, confusion and impaired motor functions.
- 12. AntiHistamines • Histamine occurin plants and animal tissue— component of some genomes and stinging secretion • Histamines+serotonin+PGs+ Interleaukins+Cytokines are called Autocoids—local Horomes. • L-Histidine— Decarboxylase—Histamine • Responsible for immidiate allergic and inflamatory reactions • Play an important role in gastric acid secretion.
- 13. Receptor Distribution Functions H1receptors 1. Airways, intestinal and uterine smooth muscles 2. Small Blood Vessels 3. Large Blood vessels 1. Contraction 2. Vasodialation 3. Vasocontriction H2 Receptors 1. Gastric. Glands 2. Blood Vessels Mast Cells 3. Brain, Cardiac muscles 1. Acid Secretion 2. Vasodialation 3. Increases Synapses H3 receptors 1. Brain 2. Lungs, Spleen Gastric Mucosa and Skin 1. Sedation 2. Reduction of histamine release H4 Receptors 1. Eosinophils, mast cells, basophils, CD4 T cells 1. Chemotaxic Effect
- 14. Clinical Pharmacological Effectof Histamine • Aerosol histamine –provocative test of Bronchial Hypersensitivity • Intra dermal injection for Triple Response(red spot, Edema, Flare) for the. Involvement of three types of cells— smooth Muscles of blood vessels, capillary or venular endothelium and sensory nerve endings. • Histamine causes Bronchoconstriction by hyperactive Neural responses in asthmatic patients. • Injection of histamine cause decrease in systolic and diastolic pressure and increase in heart rate.
- 15. ANTIHISTAMINES—Histamine Antagonists First generationAntihistamines • We’re introduced in 1930s • Chlorphenarmine I/V, I/M , PO 2-8mg ,2-5mg/5ml (OTC for Cold) • Diphenhydramine tab. 15-25mg, PO 10mg/5ml • Promethazine 5mg/5ml( Anti emetic) • Hydroxyzine 15-100mg PO • Cyclizine25-50mg PO(motion sickness) • Meclizine 25-30mg PO( motion Sickness) • Cyproheptadine 4mg PO • Peak Plasma concentration-1-2hrs • Metabolized CYP3A4 • Half life— 12-15hrs Second generation Antihistamines • Introduced in 1980s • Fexofanadine(allegra)60-180mg PO • Loratadine 10mg PO • Desloratadine 5mg PO • Citrizine 5-10mg PO ( metabololite of hydoxyzine) • Levocitrizine 5-10 mg PO • Azelastine 4mg PO, 0.28 mg Intranasally • Rupatadine 10mg PO • Peak Plasma concentration-1-8hrs • Metabolized CYP3A4 • Half life— 10-18hrs
- 16. Mechanism of actionand Uses • Block the effect of Histamines by reversible competitive antagonist at H1 receptor promotes Anticholinergics effect • HI antagonists produce effects at muscarinic, cholinoceptor, Alfa- adrenoceptor, Serotonin and local anaesthetic receptor sites • Sedation- known as asleep aides • Anti nausea and anti emetic effect • Antiparkinsonism effecct • Anti allergic reactions • Motion sickness and vestibular disturbances • Pruritis
- 17. Side Effects ofAnti Histamines • Sedation • CNS depression • Hypotension • Cardiac arrhythmias • Dry mouth, constipation, and delayed gastric emptying • Convulsions in children • Teratogenic effects with some drugs— malformation in neonates