B13 Flashcards
Paclitaxal
Microtubule stabilisation agent
MoA:
- Paclitaxel binds to the β subunit of tubulin causing hyper-stabilisation of the microtubule.
- This prevents the cell from undergoing disassembly and therefore reorganising the microtubule cytoskeleton. This adversely affects cell function, as a dynamic microtubule network is key to effective cellular transport.
Use:
- Paclitaxel is a taxoid antineoplastic agent
- Used for advanced ovarian carcinoma + breast cancer
Cisplatin
Antineoplastic alkylating agent
Use:
- Alkylating agent
- Cancer treatment
Isoniazid
Bactericidal agent
MoA:
- Isoniazid is a prodrug and must be activated by bacterial catalase.
- Once activated, isoniazid inhibits the synthesis of mycolic acids, an essential component of the bacterial cell wall. Isoniazid also disrupts DNA, lipid, carbohydrate, and nicotinamide adenine dinucleotide (NAD) synthesis and/or metabolism
Use:
- Isoniazid is a highly specific bactericidal agent, which targets mycobacterium and is ineffective against other microorganisms
Ethambutol
Bactericidal agent
MoA:
- Not fully understood but it is thought to inhibit arabinosyl transferases which is involved in cell wall biosynthesis.
Use:
- Ethambutol is an oral chemotherapeutic agent
- Apecifically effective against actively growing mycobacterium
Rifampicin
Broad spectrum bactericidal
MoA:
- Inhibition of DNA-dependent RNA polymerase, leading to a suppression of RNA synthesis and cell death.
- Importantly Rifampicin can target bacterial but not mammalian versions of the enzyme.
Use:
- Rifampicin is a broad spectrum antibiotic (targets both gram-positive and gram-negative organisms), which is easily absorbed and distributed within the body
- Due to the emergence of resistant bacteria, the use of Rifampicin is restricted to mainly mycobacterial infections
Pyrazinamide
Antibiotic
Use:
- Pyrazinamide a highly specific agent used with other drugs to treat TB
- It is active only against Mycobacterium tuberculosis and is active only at a slightly acid pH
Ciprofloxacin
Broad spectrum antibiotic (quinolone)
MoA:
- Inhibition of topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, strand supercoiling repair, and recombination
Use:
- Ciprofloxacin can be used against a wide range of gram-negative and gram-positive microorganisms
Salmeterol
Salbutamol
Beta 2 adrenergic agonist use
Use:
- B2-receptor stimulation in the lung causes relaxation of bronchial smooth muscle, bronchodilation, and increased bronchial airflow.
- They are used to manage asthma and other chronic obstructive airway diseases
Budesonide
Anti-inflammatory corticosteroid
Use:
- Crohn’s disease
- Asthma inflammation
- UC
MoA:
- Has a high glucocorticoid effect and a weak mineralocorticoid effect.
- Its binding affinity to the glucocorticoid receptor is higher than cortisol and prednisolone
Montelukast
Leukotriene receptor antagonist
Use:
- Used as an alternative to anti-inflammatory medications in the management of asthma and exercise-induced bronchospasm (EIB)
Ipratropium
Anticholinergic agent
Use:
- Bronchodilator used in the management of cholinergic-mediated bronchospasm associated with COPD
- Treatment of rhinorrhoea associated with the common cold or with allergic or non-allergic seasonal rhinitis.
Verapamil
Class IV anti-arrhythmia agent
MoA:
- Verapamil inhibits voltage-dependent calcium channels. In the heart it blocks the L-type calcium channels causing a reduction in ionotropy and chronotropy, reducing heart rate and blood pressure.
Diltiazem
Calcium channel inhibitor
Use:
- Used alone or with an ACE inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal’s variant angina
Atenolol
Atenolol has similar properties to propranolol and it is a β1-selective antagonist
MoA:
- Higher doses of Atenolol also competitively block β2-adrenergic responses in the bronchial (in asthmatic patients can cause bronchoconstriction) and vascular smooth muscles
Atropine
Antimuscarinic agent
MoA:
- Atropine binds to and inhibits the muscarinic (M2) acetylcholine receptor.
Use:
- Prevents or abolishes bradycardia, asystole and cardiac arrest