Pharmacology+perscriptions Flashcards
(105 cards)
What is ‘indication’
use of that drug for treating a particular disease
What is a ‘contracindication’
Specific situation in which a drug, procedure or surgery should not be used as it may become harmful
ACEi hypertension
Common examples: ramipril, lisinopril, enalapril
Mechanism of action: work on the renin-angiotensin system, reducing the formation of angiotensin 2 (a vasoconstrictor) which in turn causes vasodilation. Conversely, they also increase the formation of bradykinin, a peptide which is a vasodilator.
Have renal-protective effects, which is why they are always preferred first line for patients with Type 1 diabetes
Ramipril hypertension
ACEi drug
Dose range for hypertension: 1.25-10mg once daily
10% patients will develop dry cough due to increased bradkykinins – manage appropriately
Cautions (i.e. things to look out for/circumstances in which the medicine can be used but cautiously and with increased monitoring): diabetes (may lower blood glucose); first dose hypotension
Contraindications:
Common/key side effects: alopecia, angina pectoris, angioedema (more common in Afro-Carribean patients), constipation, dry cough, electrolyte imbalance (INCREASE potassium, DECREASE sodium)
Key point for practice: around 10% of patients will develop a dry cough (due to bradykinin), so please be on the lookout for this in patients who are newly prescribed an ACE inhibitor, but also those who have been prescribed it for a while as the cause of a cough may have been missed
A2RB hypertension
Common examples: losartan, candesartan, irbesartan
Mechanism of action: reversibly and competitively prevents angiotensin II binding to the AT1 receptor in smooth muscle and other tissues. This leads to relaxation of the smooth muscle, reducing blood pressure.
NOT to be combined with an ACEi in the treatment of hypertension
DOES NOT cause cough (does not increase bradykinin levels which is the cause of cough when using ACEi)
Losartan potassium (hypertension)
A2RB drug
Dose range for hypertension: 50-100mg
Cautions: Afro-Carribean patients (reduced benefit), elderly (use lower doses initially), renal artery stenosis
Contraindications: NOT to be given with the drug ‘aliskiren’ in patients with an estimated Glomerular Filtration Rate (renal function measure) of <60mL/minute or those with diabetes
Common/key side effects: abdominal pain, cough, diarrhoea, postural hypotension (more common in those also taking diuretics)
Key point for practice: the ‘potassium’ given after the drug name is the ‘drug salt’. Often drugs are formulated with another molecule to increase their solubility.
Calcium channel blockers for hypertension (Dihydropyridines)
Common examples: amlodipine, felodipine, lercanidipine, nifedipine
Mechanism of action: peripheral arterial vasodilators that work by blocking calcium influx into vascular smooth muscle (and less so cardiac muscle), which in turn reduces contraction of those muscles as cells are dependent on extracellular movement of calcium ions
Amlodipine for hypertension
Ca channel blocker (CCB)
Dose range for hypertension: 5-10mg once daily
Cautions: elderly
Contraindications: cardiogenic shock, significant aortic stenosis, unstable angina
Common/key side effects: abdominal pain, dizziness, drowsiness
Key point for practice: if a patient is recently started on amlodipine and suffers ankle swelling, the drug is the likely cause – although not always!
Thiazide diuretics
Common example: Bendroflumethiazide, indapamide (‘thiazide-like’)
Mechanism of action: inhibits sodium and chloride ion reabsorption from the distal convoluted tubules in the kidneys. Water follows ions (movement from high to low water potential) and therefore this ion movement causes increased water loss, increasing how often patients urinate. It also has an effect on vascular smooth muscle, where it is thought to dilate blood vessels.
Most hypertensive drugs cause electrolyte imbalance – thiazide decrease K+ and acei decrease K+
Bendroflumethiazide hypertenison
Thiazide drug
Dose range for hypertension: 5-10mg daily (maintenance dose)
Cautions: diabetes, gout, hyperaldosteronism, malnourishment, nephrotic syndrome, systemic lupus, elderly (use lower doses)
Common/key side effects: alkalosis hypochloraemic, constipation, diarrhoea, electrolyte imbalance (hypokalaemia in particular!)
Beta blockers hypertension
Common example: propranolol, atenolol, bisoprolol, labetalol
Mechanism of action: through action at beta-adrenergic receptors, either prevent increases in heart rate or prevent contraction of vascular smooth muscle
Some beta-blockers are classed as ‘cardioselective’; meaning can specifically target receptors in the heart
Atenolol
B blocker drug
Dose range for hypertension: 25-50mg daily
Cautions: diabetes (masks hypoglycaemic symptoms!), first-degree AV blockm, history of obstructive airway disease (can use but cautiously)
Contraindications: asthma, cardiogenic shock,
Common/key side effects: bradycardia, depression, dry eye, fatigue, peripheral coldness (due to vasoconstriction), sleep disorders
Key point for practice: we avoid beta-blockers in asthmatic patients or those with a history of bronchospasm as they cause bronchoconstriction (beta receptor action)
Statins
Common examples: simvastatin, atorvastatin, rosuvastatin
Mechanism of action: competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in cholesterol synthesis in the Liver
Myopathy (muscle toxicity) can occur with any statin and be incredibly painful and dehabilitating. Statin therapy is typically not started if the baseline creatine kinase concentration (biproduct of muscle cell turnover) is more than 5 times the upper limit of normal.
If already started treatment, if symptoms are severe discontinue (ezetimibe can be tried instead) and if creatinine kinase markedly raised then also discontinue
Simvastatin
Statin
Dose range for hypertension: 10-80mg daily at night
Cautions: elderly, high alcohol intake, history of liver disease, hypothyroidism
Common/key side effects: asthenia, constipation, dizziness, myopathy
Key point for practice: 10mg tablets can actually be purchased from a pharmacy without prescription (as a ‘Pharmacy’ medicine)
Atrovastatin
Statin
Dose range for hypertension: 10-80mg daily
Cautions: elderly, high alcohol intake, history of liver disease, hyperthyroidism
Common/key side effects: asthenia, constipation, dizziness and myopathy
Key point for practice: unlike simvastatin, the dose does not have to be taken at night although many clinicians believe it does
modified release tablets
Used where the rapid onset of a drug is not desirable or a delay is sought
The dosage form is changed so to modify the drug release profile
There are two types:
Delayed-release e.g. gastro-resistant (enteric) tablets. The drug is released at a predefined time or in a particular area of the gastrointestinal tract
Extended-release (also known as prolonged or sustained release tablets). The drug is released more slowly over a longer period, which in turn sustains drug plasma levels
Oral administration advantages and disadvantages
Advantages:
Patient preference (painless, easy, portable)
Cheap (to both manufacture and administer)
Variety of dosage forms available
High dose is possible
Can use modified release approaches
Disadvantages:
Extensive first-pass metabolism, which may require large doses to achieve the desired therapeutic effect
Food effects
Not suitable for particular patients e.g. unconscious
Drug delivery via topical patches
Transdermal patches deliver a constant and controlled dosage
Advantages:
Avoid pH variations of the GI tract
Avoid majority of first-pass metabolism
Disadvantages:
Few drugs are suitable for transdermal delivery
topical drug administration advantages and disadvantages
Advantages: Patient preference (easy, but sometimes messy e.g. ointments) Avoid pH variations of the GI tract Avoid majority of first-pass metabolism Stop absorption
Disadvantages:
Few drugs are suitable for transdermal delivery
Slow absorption
Parenteral administration
Technically, any method of drug administration that does not involve the gastrointestinal tract (enteral route); however, in practice, the term is used for administration methods via injection for example: Intravenous (also infusions) Intramuscular Subcutaneous Intra-articular Intradermal Intraspinal/intrathecal (never vinca-alkaloids e.g. vincristine & vinblastine!) Intra-arterial
types of perscription
NHS prescriptions (medicines that most patients do not pay for) FP10 – green FP10MDA – blue FP10D – yellow FP10PN and FP10SP – lilac Hospital drug charts
Private prescriptions (medicines that patients always pay for)
These can be written on anything deemed suitable by the supplying pharmacist e.g. plain white paper
FP10PCD – pink – private prescriptions for controlled drugs
Drug information included on perscription
Name of drug Dose regimen (eg 1 tablet taken daily) Quantity given Formlation eg tablets Strength
unlicensed meds
By law, before a medicine can be placed on the market, it must be given a marketing authorisation (product license) by a medicines regulator (the MHRA in the UK)
Unlicensed medicines are:
Medicines which have a license in other countries but not in the UK, so are imported
Medicines which have a UK license but need to be made up into another formulation which has no license
A medicine that has no license at all, anywhere
off label med use
If a medicine is prescribed or used ‘off-label’, this means that the medicine is being used in a different way than that described in the UK marketing authorisation (product license); for example:
Using a medicine for a different indication (condition) than that stated in its license
Using a medicine in an age group outside the licensed range
Using a medicine at a higher dose than stated in the license