9.Respiratory Pharmacology.docx

+-----------------+-----------------+-----------------+-----------------+ | **First | | | | | Generation | | | | | Histamine | | | | | An...

+-----------------+-----------------+-----------------+-----------------+ | **First | | | | | Generation | | | | | Histamine | | | | | Antagonists** | | | | +=================+=================+=================+=================+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Reversibly | **[Allergies]{. | \- Sedation | \- | | inhibits H1 | underline}** | (Cross BBB/act | Diphenhydramine | | receptors, | | on H1 in brain) | | | activation of | \- Urticaria | | -Dimenhydrinate | | which induces | | \- Dizziness | | | contraction of | \- Angioedema | | \- | | bronchioles and | | \- Tinnitus | Chlorpheniramin | | increased nasal | \- Allergic | | e | | and bronchial | rhinitis | \- Blurred | | | mucus | | vision | | | production. | **[Other]{.unde | | | | | rline}** | | | | | | | | | | \- Motion | | | | | sickness | | | | | | | | | | \- Sleep aid | | | +-----------------+-----------------+-----------------+-----------------+ | **Second | | | | | Generation | | | | | Histamine | | | | | Antagonists** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Same as | **[Allergies]{. | \- Generally, | \- Loratadine | | first | underline}** | well tolerated | | | generation, but | | | \- Fexofenadine | | do not act on | \- Urticaria | | | | muscarinic | | | \- | | receptors, | \- Angioedema | | Desloratadine | | alfa-adrenergic | | | | | receptors and | \- Allergic | | \- Cetirizine | | cannot cross | rhinitis | | | | BBB. | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mucolytics** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | [Expectorants:] | \- Common cold | \- Generally, | \- Guaifenesin, | | | | well tolerated | | | Increases | \- Pneumonia | | \- | | wateriness of | | | N-acetylcystein | | airway | \- COPD | | e | | secretions | | | | | making them | \- Cystic | | \- Dornase alfa | | easier to cough | Fibrosis | | (DNAse) | | up. | | | | | | | | | | [Mucolytics: | | | | | ] | | | | | | | | | | Breakdown mucus | | | | | chemical bonds | | | | +-----------------+-----------------+-----------------+-----------------+ | **Dextromethorp | | | | | han** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Extra | | Action** | | Effects** | Information** | +-----------------+-----------------+-----------------+-----------------+ | \- Synthetic | Antitussive | **[Mild opioid | Naloxone can be | | codeine | agent | effects when | given for | | analogue. | (suppresses | used in | overdose | | Antagonizes | cough) | excess]{.underl | | | N-methyl-d-aspa | | ine}** | | | rtate | | | | | (NMDA) | | \- Respiratory | | | glutamate | | depression | | | | | | | | receptors | | \- Constipation | | | | | | | | | | \- Euphoria | | | | | | | | | | \- Miosis | | | | | | | | | | **[Contraindica | | | | | tions]{.underli | | | | | ne}** | | | | | | | | | | \- Monoamine | | | | | oxidase | | | | | inhibitors | | | | | (MAOIs) pr | | | | | Serotonin | | | | | Reuptake | | | | | Inhibitors | | | | | (SSRIs) | | | | | (Increases risk | | | | | of serotonin | | | | | syndrome) | | +-----------------+-----------------+-----------------+-----------------+ | **α1-Adrenergic | | | | | Agonists** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Used as | \- Hyperemia | \- Hypertension | \- | | alpha 1 | | | Pseudoephedrine | | adrenergic | \- Oedema | \- CNS | | | agonist on | | stimulation/anx | \- | | smooth muscle | \- Nasal | iety | Phenylephrine | | receptors which | Congestion | | | | stimulates | | \- | \- | | phospholipase C | | Tachyphylaxis | Xylometazoline | | activity | | | | | resulting in | | | \- | | vasoconstrictio | | | Oxymetazoline | | n | | | | | and mydriasis | | | | +-----------------+-----------------+-----------------+-----------------+ | **Pulmonary | | | | | Hypertensive | | | | | Drugs** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- | \- Pulmonary | \- Hepatotoxic | **Bosentan** | | Competitively | | | | | inhibits | \- Hypertension | \- Anaemia | | | endothelin-1 | | | | | receptors, | | \- Diarrhoea | | | thereby | | | | | preventing | | \- Flushing | | | pulmonary | | | | | vasoconstrictio | | \- GERD | | | n | | | | | and decreasing | | \- Headache | | | pulmonary | | | | | vascular | | | | | resistance | | | | +-----------------+-----------------+-----------------+-----------------+ | **Pulmonary | | | | | Hypertensive | | | | | Drugs** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Inhibits | \- Pulmonary | \- Headaches | **Sildenafil** | | cGMP | hypertension | | | | phosphodiestera | | \- Feeling sick | | | se-5 | | (nausea) | | | (PDE-5), which | | | | | normally breaks | | \- Flushing | | | down nitric | | including hot | | | oxide. | | flushes | | | | | | | | \- This | | \- Indigestion | | | prolongs the | | | | | effects of | | \- Stuffy nose | | | nitric oxide, | | | | | resulting in | | \- Feeling | | | arterial | | dizzy. | | | | | | | | vasodilation. | | | | | | | | | | \- Mainly used | | | | | for erectile | | | | | dysfunction | | | | +-----------------+-----------------+-----------------+-----------------+ | **Pulmonary | | | | | Hypertensive | | | | | Drugs** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- | \- Pulmonary | \- Flushing | Epoprostenol | | Prostacyclins | hypertension | | also inhibit | | (PGI2) | | \- Jaw pain | platelet | | analogues. Have | | | aggregation | | direct | | \- Headache | | | vasodilatory | | | **Epoprostenol | | effects on | | \- Cough | and** | | pulmonary and | | | **iloprost: -** | | systemic | | \- Myalgia | | | arterial | | | | | vasculature. | | \- Diarrhoea | | | | | | | | | | \- Vomiting | | | | | | | | | | \- Nausea | | +-----------------+-----------------+-----------------+-----------------+ | **Adrenergic β2 | | | | | Receptor | | | | | Agonists** | | | | | | | | | | Long-Acting | | | | | Beta 2 Agonists | | | | | (LABAS) | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | **[Bronchodilat | \- Asthma | \- Increased | \- Albuterol | | ion]{.underline | | heart rate | | | }** | | | \- Salmeterol | | | | \- Headache | | | \- On β2 | | | \- Formoterol | | receptors found | | \- Dizziness | | | on lungs, it | | | | | facilitates | | \- Anxiety | | | conversion of | | | | | adenylate | | \- Rash | | | cyclase (AC) to | | | | | cAMP, which | | \- Tremors | | | relaxes | | | | | bronchial | | | | | smooth muscle | | | | | by inactivating | | | | | myosin light | | | | | chain kinase | | | | | and decrease | | | | | intracellular | | | | | calcium. | | | | +-----------------+-----------------+-----------------+-----------------+ | **Muscarinic | | | | | Antagonists** | | | | | | | | | | Long-Acting | | | | | Muscarinic | | | | | Antagonists | | | | | (LAMAS) | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- | \- COPD. | \- Bronchial | \- Ipratropium | | Competitively | | vasodilation | | | inhibit | \- Asthma | | \- Tiotropium | | acetylcholine | | **[Contraindica | (long acting) | | binding on | | tion]{.underlin | | | muscarinic | | e}** | | | receptors (M3), | | | | | preventing | | [\< 12 years | | | bronchoconstric | | old]{.underline | | | tion. | | } | | | | | | | | Tiotropium is | | \- Glaucoma | | | long acting | | | | | | | \- Urinary | | | | | retention | | +-----------------+-----------------+-----------------+-----------------+ | **Inhaled | | | | | Corticosteroids | | | | | ** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | Inhibit the | \- Chronic | \- Oral | \- Prevented by | | synthesis of | asthma | candidiasis | rinsing mouth | | virtually all | | (thrush) | following | | cytokines. | | | administration | | Inactivate | | \- Hoarse voice | prevents oral | | NF-κB, which is | | | candidiasis | | the | | \- Dysphonia | | | transcription | | | | | factor that | | \- Altered | | | induces the | | taste | | | production of | | | | | TNF-α and other | | | | | inflammatory | | | | | agents | | | | +-----------------+-----------------+-----------------+-----------------+ | **Anti-leukotri | | | | | enes** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Examples** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | **[Zileuton]{.u | \- COPD. | **[Montelukast] | \- Zileuton | | nderline}** | | ** | | | | \- Asthma | | \- Montelukast | | 5-lipoxygenase | | \- Arthralgia | | | pathway | | | \- Zafirlukast | | inhibitor. | | \- Bruising | | | Blocks the | | | | | conversion of | | \- Dyspepsia | | | arachidonic | | | | | acid to | | \- Excessive | | | leukotrienes | | thirst | | | (bronchoconstri | | | | | ction | | **[Zafirlukast] | | | mediators). | | ** | | | | | | | | **[Montelukast, | | \- Arthralgia | | | zafirlukast]{.u | | | | | nderline}** | | \- Bruising | | | | | | | | Competitively | | \- GI upset | | | inhibit | | | | | leukotriene | | **[Contraindica | | | receptors | | tions]{.underli | | | (CysLT1) on | | ne}** | | | bronchial | | | | | smooth muscles. | | [Zafirlukast]{. | | | | | underline} | | | | | | | | | | Liver | | | | | impairment | | | | | | | | | | Renal | | | | | impairment | | +-----------------+-----------------+-----------------+-----------------+ | **Omalizumab** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Monoclonal | \- Severe | \- Headache | when asthma is | | anti-IgE | chronic Asthma | | refractory to | | antibody. | | \- Skin | long-acting β | | | | reactions | 2-agonists and | | \- Binds | | | inhaled | | unbound serum | | \- Cough | corticosteroids | | IgE at the Fc | | |. | | region (FcεRI) | | \- Anaphylaxis | | | | | (rare) | | +-----------------+-----------------+-----------------+-----------------+ | **Methylxanthin | | | | | es** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Inhibits | \- COPD | [Neurotoxicity] | \- | | phosphodiestera | | | Theophylline. | | se, | \- Asthma | | | | which normally | | \- Seizures | | | hydrolyses | | | | | cAMP. | | [Cardiotoxicity | | | | | ] | | | \- This | | | | | increases cAMP | | \- Tachycardia | | | levels, | | | | | resulting in | | \- Arrhythmias | | | bronchodilation | | | | |. | | \- Metabolized | | | | | by cytochrome | | | \- Also blocks | | P-450. | | | the actions of | | | | | adenosine, | | | | | thereby | | | | | preventing | | | | | bronchoconstric | | | | | tion | | | | +-----------------+-----------------+-----------------+-----------------+ | **Magnesium | | | | | Sulphate** | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Inhibits | \- Asthma | \- Hypotension | \- Also used as | | calcium influx | | | laxative | | into airway | | \- ECG changes | | | smooth muscle | | | | | cells, thereby | | \- GI upset | | | decreasing | | | | | airway tone. | | \- Urinary | | | | | retention | | | | | | | | | | \- Sedation | | | | | | | | | | \- Confusion | | | | | | | | | | **[Contraindica | | | | | tions]{.underli | | | | | ne}** | | | | | | | | | | \- Certain GI | | | | | disease | | +-----------------+-----------------+-----------------+-----------------+ | **Methacholine* | | | | | * | | | | +-----------------+-----------------+-----------------+-----------------+ | **Mechanism of | **Uses** | **Side | **Information** | | Action** | | Effects** | | +-----------------+-----------------+-----------------+-----------------+ | \- Muscarinic | \- Used in | \- Shortness of | **[Methacholine | | receptor (M3) | bronchial | breath | challenge | | agonist. Causes | provocation to | | test]{.underlin | | bronchoconstric | help diagnose | \- Wheezing | e}** | | tion | asthma | | | | | | \- Coughing | \- Has high | | | | | sensitivity but | | | | \- Dizziness | low specificity | | | | | | | | | \- GI upset | | | | | | | | | | \- Chest pain | | | | | | | | | | **[Contraindica | | | | | tions]{.underli | | | | | ne}** | | | | | | | | | | \- Recent heart | | | | | attack | | | | | | | | | | \- Recent | | | | | stroke | | | | | | | | | | \- Uncontrolled | | | | | hypertension | | | | | | | | | | \- Severe lung | | | | | disease | | | | | | | | | | \- Aortic | | | | | aneurysm | | +-----------------+-----------------+-----------------+-----------------+