Respiratory Drugs Table PDF

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Summary

Respiratory Drugs Table...

Description

Drug Class Bronchodilators (Releivers)

Sub Class

Types Short Acting (SABA)

Example Salbutamol

Mechanism of Action Stimulate bronchial smooth muscle B2adrenoceptors. ↑cAMP  ↑PKA  Relaxation Act rapidly (max effect 30 mins)

Used For 1st line for mild intermittent asthma (Reliever)

B2- adrenoceptors agonists

Long Acting (LABA)

Salmetarol

Stimulate bronchial smooth muscle B2adrenoceptors. ↑cAMP  ↑PKA  Relaxation NOT for acute relief Antagonise Cysteinyl leukotriene receptors. CysLTs (LTC4, LTD4 and LTE4) derived from inflammatory cells  contraction of ASM, Oedema, ↑mucus, ↑eosinophils. Relax ASM. Low therapeutic ratio (good efficacy) Signal via nuclear receptors, bind to glucocorticoid response elements (GRE)  gene transcription (↑anti-inflammatory, ↓inflammatory). ↓cytokines, prevent IgE antibody production, ↓mast cells, prevent allergen influx Direct into lung  all the above effects where you want it Mast Cell Stabiliser (suppress histamine release), weak anti-inflammatory effect, reduction of cytokine release

Nocturnal Asthma Add on therapy (must be co-admin with glucocorticoid.) Asthma (antiinflammatory) Add on therapy. Used in Exercise induced Asthma

CysLT1 Receptor Antagonists

Antiinflammatory (controllers/preve ntors)

Corticosteroids (Glucocorticoids)

Cromones

IgE antibodies

Antiinflammatory and Bronchodilator

Montekulast Zafirlukast

Oral Steroid

Prednisolone

Inhaled Steroid Inhaled

Beclomethasone

Antiinflammatory anti-IgE monoclonal antibody

Omalizumab (Injection every 24 weeks  v.expensive).

Inhibits the binding to high affinity IgE receptor and inhibits mediator release from basophils and mast cells. No effect on pulmonary function but ↓exacerbations.

Theophylline (oral)

Non-selective inhibition of phosphodiesterase (PDE). Inhibits PDE3 and increases cAMP in ASM  relaxes ASM. Anti-inflammatory actions, inhibit mediator release from mast cells, increased mucus clearance. Non-selective PDE inhibitor (↑cAMP)  relaxes ASM Ipratropium (non-selective blocker of M1, M2, M3 receptors. M3 muscarinic receptors mediate contraction of ASM.

Methylxanthines

Cromoglicate

Aminophyline (IV) Bronchodilators

Competitive muscarinic receptor antagonists (all given via inhalation)

Short Acting muscarinic antagonists (SAMAs)

Ipratropium Oxitropium

Asthma to suppress immune system (Step 5 treatment)

Side Effects When inhaled: fine tremor, tachycardia, arrhythmias, hypokalaemia.

Contraindications Use with caution in hyperthyroidism, CVS disease, arrhythmias and hypertension. NB: Do not prescribe non-selective beta blockers in asthma (bronchospasm).

Well tolerated. But headaches and GI upset reported e.g. abdo pain Oral Candidiasis, GI - peptic ulcer, MSK – myopathy, endocrine – Cushing’s

Asthma – maintenance therapy Prophylaxis in mild and exercise induced asthma not used much due to poor efficacy Prophylaxis in Asthma  with raised IgE and severe persistant allergic asthma despite max therapy

Fewer systemic side effects v.little systemic absorption

Abdo pain, headache, pyrexia

Caution in autoimmune disease

Asthma (maintenance therapy)

P450 drug interactions e.g. erythromycin

Asthma (acute attacks)

Narrow therapeutic window and has adverse effects at toxic range (arrhythmias, seizures, hypotension)

COPD – palliative to reduce exacerbations. Or as LAMA/LABA combo. Or as triple therapy

High therapeutic ratio. Not well systemically absorbed

Long Acting Muscarinic Antagonists (LAMAs) Antiinflammatory Mucolytics

PDE4 inhibitors

Tiotropium Aclidinum

Tiotropium selective for M3. Longer ½ life than ipratropium.

ICS/LABA/LAMA. Short term relief.

therefore few side effects

Rofumilast (oral)

Selective PDE4 inhibitor. PDE4 = expressed in neutrophils, T cells and macrophages.

To reduce COPD exacerbations (additive to LABA or LAMA) Reduce sputum viscosity (Add on therapy)

Nausea, Diarrhoea/headac he/weight loss Rarely GI bleeding

Syptomatic treatment of acute exacerbations of chronic bronchitis

Very rarely; nausea, vomiting, diarrhoea, abdo pain

Oral Carbocisteine Oral Erdosteine

Caution: those with history of peptic ulcer Active peptic ulcer See above...