DRUGS Monday, 17 January 2022 5:17 PM PEDIATRICS VIVA-VOCE: DRUGS -Dr.Ashray S Patel Ph No: 9482141673 E-mail: patel1995ash@gmail.com ANTIPYRETICS ANTHELMINTICS ANTIBIOTICS ANTICONVULSANTS ANTIEMETICS ANTIHISTAMINES INOTROPES BRONCHODILATORS ANTIPYRETICS: 1) PARACETAMOL: • ACETAMINOPHEN • MoA: COX-3 inhibitor • Used to control fever as well as for mild to moderate pain such as myalgia, headache. Closure of PDA in neonates. • Dosage: 15mg/kg/dose ORAL 15mg/kg/dose RECTAL 10mg/kg/dose IV Maximum of 90mg/kg/day or 4g/day oral & 60mg/kg/day IV • Toxic dose: 200mg/kg or 10g • Antidote: N-Acetylcysteine • Formulations available: Syrup: 125mg/5ml or 250mg/5ml Tablet: 500mg Rectal Suppository: 125mg/250mg • Adverse effects: safe and well tolerated drug. Hepatic damage. 2) MEFENAMIC ACID: • MoA: Reversible COX inhibitor with PG receptor antagonist action as well. • Antipyretic, analgesic and good efficacy in dysmenorrhea • Dosage: Antipyretic: 5-8mg/kg/dose 8 hourly Analgesic: 25mg/kg/day 8th hourly • Formulations available: Syrup: 100mg/5ml Tablet: 250/500mg • Adverse effects: Diarrhea, Skin rashes 3) IBUPROFEN: • MoA: Reversible COX inhibitor. • Safest NSAID • Dosage: 5-10mg/kg/dose 6-8 hourly maximum of 40mg/kg/24hr. • Formulations: Syrup: 125mg/5ml or 100mg/5ml • Adverse effects: much less compared to aspirin ANTHELMINTICS: 1) ALBENDAZOLE: • Broad spectrum anthelminthic • MoA: alters cytoskeletal structure formation • Due to its broad spectrum activity, indicated for deworming. • Deworming done twice a year by Indian Government. • National deworming day is on February 10th. In regions with high prevalence, 2nd round of deworming is carried out on 10th August. • Age group included is from 1 to 19 years. • Dose: 200mg for children under 2 years and 400mg for the rest. • Formulation: 400mg in 10ml suspension is available. ANTIBIOTICS: 1) AMIKACIN: • Aminoglycosides • MoA: Inhibit peptide synthesis. • Exhibits concentration dependent killing and post-antibiotic effect, hence given once daily. • Main action against gram negative, aerobic bacilli. • Dose: 15-29mg/kg/day given IV • Side effects: Nephrotixicity, ototoxicity. 2) AMPICILLIN: • Extended Spectrum Penicillins • MoA: Inhibits cell wall synthesis • Effective against gram positive cocci and bacilli, along with few gram negative organisms. • Usually given IV, though oral formulation given. • Dose: 100-200mg/kg/day 6th hourly, 200-400mg/kg/day for meningitis. • Side effects: hypersensitivity reactions 3) AMOXICILLIN: • Similar to Ampicillin • Usually given orally • Cannot be used for meningitis • Dose: 25-50mg/kg/day given 8 to 12th hourly orally, 50-100mg/kg/day IV • Formulations: Syp as 125mg/5ml, 250/500mg tablets • CLAVULINATE: B-latamase inhibitors. Hence combination is effective against B-lactamase producing organisms. • Formulation: 156mg/5ml, 228mg/5ml, 457mg/5ml, 375mg tablets, 625mg tablets. 4) CEFTRIAXONE: • Third generation Cephalosporin • Resistant to B-lactamase producing organisms . • Highly effective against Gram negative cocci and bacilli, anaerobes • Dose: 50-75mg/kg/day q 12-24hourly, meningitis 100mg/kg/day. • Given IV • Side effects: Hypersensitivity reactions, pseudomembranous colitis, diarrhoea 5) CEFIXIME: • Third generation Cephalosporin • Given orally • Dose: 8mg/kg/day once or twice daily. For enteric fever, 20mg/kg/day. • Formulations: 200/400mg tablets, 50 and 100mg/5ml syp 6) VANCOMYCIN: • Glycopeptide • MoA: Inhibiton of cell wall synthesis • Effective against aerobic as well as anaerobic gram positive species. • Use is limited to treatment of serious infections caused by MRSA organisms or PMC not controlled by metronidazole. • IV • Dose: 40mg/kg/day 6th hourly & 60mg/kg/day for CNS Infections • Side Effects: RED MAN SYNDROME due to histamine release 7) AZITHROMYCIN: • Macrolide • MoA: Inhibit protein synthesis • Used to treat mainly Atypical organisms like Mycoplasma, ureaplasma, chlamydia, Moraxella, H influenza, B pertussis, STD’s • Given orally • Dose: 10mg/kg/day on empty stomach on day 1 followed by 5mg/kg/day during next 4 days. Maximum of 500mg • Side effects: allergic reactions, QT prolongation, cholestatic hepatitis 8) ANTI TUBERCULOSIS TREATMENT: • First line drugs: ISONIAZID / RIFAMPICIN / PYRAZINAMIDE / ETHAMBUTOL • All are bactericidal accept ethambutol which is bacteriostatic. • Drug Regimen: • Drug Dosage and Fixed Drug Combination: • Pyridoxine & Role of Steroids: • Side Effects: 9. COTRIMOXAZOLE: • Sulphonamides • MoA: inhibition of Bacterial Folic Acid Synthesis • Active against gram negative organisms, anti-malarial, Toxoplasmosis • Clinical Uses: UTI/Prevention of UTI, Respiratory Tract Infections / Prevention, Typhoid, STD, Dysentry • Dose: 5-8mg/kg of TMP, 25-50mg/kg of Sulfamethoxazole. Typhoid its 10mg/kg & Pneumocystis 20mg/kg. Prophylaxis against UTI is 1-3mg/kg and PCP 5mg/kg. • Formulation: 40mg/200mg per 5 ml Syp, 80mg/400mg tablet • Side Effects: Kerinecterus in newborn, hypersensitivity, crystalluria ANTICONVULSANTS: 1. LORAZEPAM / MIDAZOLAM: • Benzodiazepines • MoA: Enhance the frequency of GABA mediated Cl channel opening • Clinical use: First line agent in Status Epilepticus • Dose: 0.2mg/kg IM or Intranasal spray 0.3mg/kg Midazolam or 0.1mg/kg/dose IV Lorazepam • Side effects: Pronounced sedative effects, development of tolerance to their anticonvulsant effects. 2. Levetiracetam • Newer Anti-epileptic drugs • MoA: by inhibiting the synaptic vesicles containing Glutamine to fuse • Broad Spectrum Anti Seizure Medication • Dose: 20-60mg/kg/day • Formulation: 100mg/mL syrup, 250/500mg tablet • Side effects: dizziness, weakness, suicidal tendencies 3. Phenytoin: • MoA: decreasing Glutamate release • Mainly used to treat GTCS type convulsions. First line drugs in status epilepticus. • Should not be used for Absence seizures or myoclonic seizures • Also used to treat Trigeminal neuralgia and ventricular arrhythmia • Dose: 5-8 mg/kg/day • Formulation: 30mg/5ml syrup, 100mg tablet • Side effects: gingival hyperplasia, megaloblastic anemia, vitamin k deficiency, hirsutism, congenital malformations 4. Valproate: • MoA: decreasing release of glutamate and increase GABA activity • Broad spectrum activity: GTCS, absence seizures, myoclonic jerks, infantile spasms, first line drugs in status epilepticus. • Dose: 20-60 mg/kg/day • Formulation: 200mg/5ml syrup, 200/400/500mg tablet • Side effects: hepatotoxic, pancreatitis, thrombocytopenia, GIT, alopecia, tremors. 5. Phenobarbitone: • Barbiturates class of drugs • MoA: enhances GABA mediated inhibitory effects and also inhibits glutamate mediated excitatory effects • Used for GTCS type and neonatal seizures • Dose: 3-5 mg/kg/day 12 hourly • Formulation: Syp available as 20mg/5ml. • Side effects: sedative, drug interaction p, irritability, hyper excitability Newer Anti-epileptics: Vigabatrine, Lamotrigine, Levitiracetam, Tigabaine, Topiramate, Zonisamide, etc ANTIEMETICS: 1. Ondansetron: • Selective 5-HT3 receptor antagonists • MoA: blocking 5-HT3 receptors peripherally on vagal nerve terminals & centrally on NTS & CTZ. • Dose: IV: 0.15mg/kg/ dose maximum 8mg/dose, can be given 4th hourly. Oral, <4yr: 2mg q4hr, 4-11yrs: 4mg q4hr, >12yrs: 8mg q4hr. • Formulation: 2mg/5ml syrup, 4mg & 8mg tablets • Side effects: very good safety profile. Headache, constipation, rashes. ANTIHISTAMINES: 1. Cetirizine: • Second generation antihistamine • MoA: H1 receptor blocker • Allergic rhinitis, urticaria • Dose: 6mo-2yr: 2.5mg OD, 2-6yrs: 2.5mg bd or 5mg od, >6yrs: 5-10mg od/bd. Avoid in children less than 6months • Formulation: 5mg/5ml Syp • Side effects: sedation, antimuscarinic side effects. 2. Chlorpheniramine maleate: • First generation antihistamine • MoA: H1 receptor blocker • Common cold • Dose: 0.35mg/kg/day q6hr • Formulation: Sinarest-AF drops(2.5mg/1ml), Sinarest AF Syp(5mg/5ml) 3. Pheniramine maleate: • First generation antihistamine • Dose: 0.5mg/kg/day q8hr • Formulation: Avil 22.75mg as 2mg ampoule INOTROPES: BRONCHODILATORS: