Pharmacology Flashcards
What is the role of ACE inhibitors?
Reduce the blood volume and cause vasodilation, therefore decreasing peripheral vascular resistance
Examples of ACEi
Ramipril Perindopril Enalapril Lisinopril Catopril
When are ACEi indicated?
(1st line) Hypertension
(1st line) Heart failure
Early renal failure with proteinuria
Secondary prevention after MI
What is the mechanism of ACEi?
Competitively inhibit ACE and reduce the generation of ATII, and consequently aldosterone. This reduces Na and H2O retention.
What are the additional effects ACEi?
Reduced ATII in tissue also leads to arterial and venous dilation. No reflex tachycardia, inhibits bradykinin breakdown (a vasodilator so further increases vasodilation) and ATII is associated with arterial and ventricular hypertrophy in hypertension, which is now prevented.
Pharmacokinetics of ACEi?
Usually a prodrug, active forms are water soluble so poor absorption in the gut. Converted to active form in the liver and most forms are excreted unchanged by the kidneys with generally short half lives.
ACEi side effects?
Persistent dry cough Postural HTN Renal impairment Disturbances to taste, nausea, vomiting, dyspepsia and bowels Angioedema
ACEi cautions
Careful in conjunction with drugs that raise potassium, at risk of hyperkalaemia
Never prescribe with NSAIDS and thiazides diuretics altogether
What are the two main types of analgesics?
NSAIDs and opioids
What are less frequent forms of analgesics?
Tricyclic antidepressants (amitriptyline)
Anticonvulsants (carbamazepine)
Diazepam
Examples of NSAIDs
Paracetamol Ibruprofen Diclofenac Naproxen Celecoxib
Examples of opioids
Codeine Morphine Fentanyl Diamorphine Tramadol
What are NSAIDs indicated for?
Mild to moderate pain, particularly MSK
Fevers
Arthritis
Ankylosis spondylitis
What are opioids indicated for?
Moderate to severe pain such as childbirth, peri operative pain and cancer
How do NSAIDs work?
Prostaglandins are cell signalling molecules involved in the inflammatory and pain responses, synthesised by arachidonic acid from COX enzymes. NSAIDs inhibit COX enzymes to reduces inflammatory and pain responses
How do opioids work?
Opioids act of 3 receptors of the CNS - μ, κ & δ. There are 2 subtypes of μ receptor. Type 1 reduces sensation of pain by inhibiting the transmission of pain signals ascending the spinal cord. Type 2 produces the unpleasant side effects of opioids.
What are the side effects of NSAIDs?
Gastric ulcers
Reduced renal perfusion (if have prior liver, kidney or cardio problems)
Hypersensitivity
Increased bruising and bleeding
What are the side effects of opioids?
Constipation Drowsiness Nausea Vomiting Respiratory arrest
Cautions for NSAIDs?
Can cause bronchospasm in asthmatics
Cautions of opioids?
Elderly
Asthmatics
Mental illness
CVD
Can be addictive
What type of drug is amiodarone?
Anti-arrhythmic
What is amiodarone indicated for?
Paroxysmal supraventricular tachycardia Nodal and ventricular tachycardia AF + flutter Ventricular fibrillation Tachyarrhythmias associated with WPW syndrome
What is the mechanism for amiodarone?
Amiodarone blocks K+ channels prolonging the refractory period, blocks Na+ with a high affinity for inactivated channels, non-competitively blocks α and β receptors resulting in anti-adrenergic effects, weakly blocks Ca2+, slows down sinus rate and AV conduction, slightly prolongs QT intervals and can cause peripheral vasodilation
Is the half life of amiodarone long or short?
Very long - gives rise to potentially serious drug interactions
Side effects of amiodarone
Corneal micro deposits Thyroid function Hepatotoxicity Pulmonary toxicity Peripheral neuropathy
Cautions of amiodarone?
In pregnancy can possibly cause neonatal goitre
Avoid in breastfeeding
CI in cardiac issues and iodine sensitivities
Examples of ARBs
Candesartan
Irbesartan
Valsartan
(-sartan suffix)
What are ARBs indicated for?
Second line treatment for:
Hypertension, heart failure and post-MI
Diabetic nephropathy
Mechanism of ARBs?
Selectively inhibits ATII at AT1 receptors.
ATII binding causes vasoconstriction, aldosterone release, sympathetic activation, potentially harmful CV effects. Antagonists cause vasodilation and blocking of aldosterone release
Cautions of ARBs?
May not be as beneficial in Afro-Caribbean Aortic/mitral stenosis Elderly Hypertrophic cardiomyopathy History of angioedema 1ο aldosteronism Renal artery stenosis
CI with aliskirin
Potentially serious interactions with many drugs
Avoid in pregnancy and breast feeding, caution in renally impaired.
How do hanging histamines work?
They are an antagonist to the histamine H1 receptor
When are anti-histamines effective?
Against mast cell activated inflammatory reactions
What type of antibiotic Trimethoprim?
Folic acid inhibitor
What is Trimethoprim indicated for?
Pneumonia (often in conjunction with sulphonamide - coxtrimoxazole)
RTI
UTI
What are the side effects of Trimethoprim?
N+V, rashes, meh oblast is anaemia (folate deficiency)
Is Trimethoprim broad spectrum? What is it effective against?
Yes it is a broad spectrum antibiotic
It is effective against gram positive and gram negative bacteria
What type of antibiotic is Penicillin?
β-lactam
Give examples of penicillin antibiotics
Penicillin, amoxicillin, flucoxicillin, benzylpenicillin
What are the side effects of penicillin?
Not many, hypersensitivity and n+v
Is Penicillin broad spectrum? What is it effective against?
Very much broad spectrum
Effective against gram positive and negative bacteria