Pharmo Flashcards
What is the difference between Parkinsonism and parkinsons disease?
- Parkinson’s disease- a degenerative disorder
- Parkinsonism- due to other causes e.g. long term use of anti- psychotic drugs
What are the 4 mechanisms of action in Parkinson’s drugs?
- Direct dopamine agonists
- pre-cursor to dopamine
- reduce dopamine metabolism
- cause local release of dopam
Drugs used in Parkinsons?
Amantadine
Levodopa
MAO-B inhibitors
Dopamine agonists e.g. bromocriptine, ropinirole, pergolide
What is the function of amantiadine in parkinsons?
Amantadine - antiviral which increases CNS dopamine release.
What is the function of Levodopa in parkinsons?
can cross the BBB. Good response initially but usually declines with time
What is the function of Dopamine agonists in parkinsons?
e.g. bromocriptine, ropinirole, pergolide.
Monotherapy in early disease/ young patients. Given with levodopa in more advanced diseas
What is the function of MAO-B inhibitors in parkinsons?
eg selegiline.
Inhibits the metabolism of dopamine, NOT levodopa.
What is the function of Entacapone in parkinsons?
- inhibits the metabolism of levodopa which happens peripherally
Side effects of Dopamine agonists in Parkinsons
Dopamine agonists- ropinirole (non ergot derivative), pergolide, cabergoline, lisuride, bromocriptine (ergot derivatives):
- ergot derivatives- fibrotic reactions in the chest, abdo, heart
- Non ergot derivative- leg oedema
- Nausea, dizziness, vivid dreams, visual distrubances, postural hypotension
Side effects of Levodopa in Parkinson
levodopa is metabolised to dopamine- good thing in the brain but peripherally the dopamine results in adverse effects e.g. nausea and vomiting. To counteract this a decarboxylase inhibitor is given with levodopa e.g carbidopa. Carbidopa does not cross the BBB so only the peripheral dopamine is metabolised to reduce side effects.
- dyskinesias- overactivity in the dopaminergic pathways, hypotension
Side effects of?
• Selegiline-
• Entacapone-
• Amantadine-
- Selegiline- gastrointestinal upset, can induce confusion
- Entacapone- gastrointestinal upset, can induce confusion
- Amantadine- not frequently used, antiparkinsonian effects weak
2 Common drugs for depression
Tricyclic antidepressants - block presynaptic reuptake of noradrenaline and serotonin
Selective serotonin reuptake inhibitors (SSRIs)- inhibit serotonin reuptake by post-synaptic nerve terminals
Examples of SSRIs
• Fluoxetine- well absorbed from the gut, metabolite is equipotent, can build up in hepatic or renal failure
• Setraline- shorter elimination half-life
• Citalopram, paroxetine
Affects of SSRIs on Depression
- Can take 6-8 weeks to start to work fully
- No sedative effect with less of an affect on cardiac conduction too.
- Better tolerated in overdose
- Should not be given to under 18s as can cause suicidal behaviour and thoughts
- Adverse effects: anorexia and weightloss, hyponatraemia, sexual dysfunction
Affects of Tricyclic antidepressants
- E.g. amitriptyline – absorbed in gut but can slow down gut motility and make its absorption slower too. Slow half-life
- Work quicker- 2 weeks
- Some e.g. amitriptyline are sedative- can be useful side effect
- Also used for treatment of neuralgia
- May exacerbate epilepsy
- Can cause weight gain
NOTE: tricyclic antidepressants also block muscarinic, histamine and alpha1-adrenoreceptors. The anticholinergic effects of this include constipation, urinary retention, tachyarrhythmias
TRUE OR FALSE
TRUE
tricyclic antidepressants are used in
- epilepsy
- prostatic hypertrophy
- Immediately after MI
- Glaucoma
TRUE OR FALSE
FALSE- its contraindicated in
Drugs in Asthma?
• Short acting beta agonist SABA - e.g. salbutamol, trade name; e.g Ventolin “the blue one” or terbutaline
• Inhaled steroid- beclomethasone, trade name: e.g. clenil modulate “the brown one”
• Long acting beta agonist LABA- e.g. salmeterol trade name: e.g. serevent, maybe “the green one” or formoterol
• Adjuncts- montelukast, theophylline, beta 2 agonist tablets • Oral steroids- prednisolone
What is Ventolin?
salbutamol, a short acting beta agonist
WHat is Clenil modulate?
beclomethasone, inhaled corticosteroid
WHat is serevent?
salmeterol, long acting beta agonist
WHat is seretide?
salmeterol (LABA) and fluticasone (steroid
Asthma – acute management- know your severities!
- Oxygen- ____ high flow non-rebreather mask
- Salbutamol- inhaled through a______
- High doses of systemic steroids e.g. oral prednisolone or IV hydrocortisone
• Ipratropium bromide (add to salbutamol nebuliser in those with acute severe or life threatening asthma or those who have little response to b2 agonists)
• ________ _______- a single IV dose ( in those with acute severe asthma or who have not had a response to intial bronchodilator therapy
- Oxygen- 100% high flow non-rebreather mask
- Salbutamol- inhaled through a nebuliser
- High doses of systemic steroids e.g. oral prednisolone or IV hydrocortisone
• Ipratropium bromide (add to salbutamol nebuliser in those with acute severe or life threatening asthma or those who have little response to b2 agonists)
• Magnesium sulphate- a single IV dose ( in those with acute severe asthma or who have not had a response to intial bronchodilator therapy
COPD: general medication for breathlessness and exercise?
Short acting beta 2 agonist as required
Short acting muscarinic antagonist as required
COPD: if the patient has exacerbation or peristent breathlessness with
FEV >50%
What drugs would you give?
Long acting beta 2 agonist
Long acting musariniv antagonist (discontinue SAMA)
COPD: if the patient has exacerbation or peristent breathlessness with
FEV < 50%
What drugs would you give?
Long acting beta 2 agonist plus inhaled corticosteroids
Long acting muscarininc antagonist (discontinue SAMA)
COPD: if the patient has persistent exacerbation or breathlessness with
What drugs would you give?
Long acting muscarinic antagonists plus long acting beta 2 agonist plus inhaled corticosteroid
Medication used for Tuberculosis?
Think of RIPE
- Rifampicin- Top 2 for 4 months
- Isoniazid- Top 2 for 4 months
- Pyrazinamide
- Ethambutol
All for 2 months
Drugs used for hypetension?
ACE inhibitors (ramipril)
Calcium- channel blcokers
thiazide type diuretics
beta blockers
Hypertension drugs- side effects
• ACE inhibitors –
• Calcium channel blockers –
• Thiazide diuretics-
• Beta-blockers-
• ACE inhibitors – dry cough (bradykinin production), severe hypotension- in RAS, first dose, heart failure, hyperkalaemia
• Calcium channel blockers –cause smooth muscle to relax so result in facial flushing, ankle swelling, headaches and dizziness
• Thiazide diuretics- dehydration, hypokalaemia/hyponatraemia/hypocalcaemia, impaired glucose tolerance/diabetes
• Beta-blockers- bradycardia/heart block, bronchospasm (do not give to asthmatics), peripheral vasoconstriction
3 main management for heart failure?
ACE inhibitors
Diuretics
Nitrates
What does ACE inhibitors for heart failure?
- blocks RAAS activity
- vasodilator so reduces afterload Can use an ARB if ACE inhibitor not tolerated though not as effective
• Falling Cardiac output • Falling blood pressure • Increased RAAS activity
What does diuretics for heart failure?
For reducing fluid retention e.g. furosemide e.g. bendoflumethiazide e.g. spironalactone
• Increased preload • Restores cardiac output in the short term
What does NITRATEs for heart failure?
Venodilators – reduce the preload on the heart. Effective in acute heart failure e.g. IV isosorbide dinitrate
• Raises BP • Increases afterload
What does loop diuretics do?
inhibit the resorption of chloride in the ascending limb of the LOH. Chloride loss also leads to loss of sodium and thus water too
Used in moderate to severe heart failure
What does Thiazide diuretics do?
inhibit sodium absorption at the DCT and water is lost with the sodium. However the major effects is from vasodilation not diuresis
Used alone in mild heart failure
What does Potassium-sparing diuretics do?
act in DCT at sodium/potassium exchange- spironolactone is an aldosterone antagonist and causes potassium retention and sodium loss. Amiloride actually interferes with sodium/potassium exchange
Used in severe congestive heart failure (usually with ACE inhibitors and loop diuretics)
Management for ischaemic heart disease (ACUTE)
think MONA
- M-morphine (+anti-emetic)
- O- oxygen
- N- nitrates (sub-lingual glyceryl trinitrate)
- A- aspirin (oral and providing no contraindication)
Ischaemic heart disease
• Everyone who has had an MI should go home on 4 medications
What are they?
Statin
- Aspirin
- Ramipril
- Bisoprolol
- +/- clopidogrel
What is APFEL score?
-Female -History of travel sickness -Non-smoker -Opioids scheduled in the post-op period
The Apfel simplified score includes female gender, history of PONV and/or motion sickness, non-smoking status, and postoperative use of opioids. When 0, 1, 2, 3, or 4 factors are present, the risk of PONV is 10%, 20%, 40%, 60%, or 80%, respectively (ROC-AUC=0.69
Name the drugs used for nausea and vomiting?
- Anticholinergics
- Antihistamines-
- Phenothiazines-
- Dopamine receptors antagonists
- Domperidone
- 5-HT antagonist
Functions of Anticholinergics and Antihistamines
- Anticholinergics- act on the vomiting centre but also affect the gastrointestinal tract directly e.g. hyoscine. Have anticholinergics side-effects e.g. dry mouth
- Antihistamines- act on H1 receptors in the vomiting centre but also have some anticholinergic power and can cause drowsiness. Newer non-sedating antihistamines have been found to not be as effective but can be useful in treating motion sickness or vestibular disease e.g. promethazine
Diabetes type 2 management
Describe monotherapy, dual therapy, triple therapy for type 2 Diabetes
Antibiotics 1- Cell wall- CCP
___________ and ____________ act on the cell wall of the bacteria – the contain a b_________ _______ and can inhibit the formation of _____________ cross-links in bacterial cell walls. Once the cell wall has been weakened water enters and the cell ______
• Penicillins and cephalosporins act on the cell wall of the bacteria – the contain a beta-lactam ring and can inhibit the formation of peptidoglycan cross-links in bacterial cell walls. Once the cell wall has been weakened water enters and the cell bursts
Examples of Cephalosporins and Penicillins
- Cephalosporins • Different generations e.g. cefotaxime, cefuroxime, cephalexin
- Penicillins • E.g. amoxicillin, flucloxacillin, benzyl penicillin, penicillin V, piperacillin • Allergies
What is amoxicilin used for?
chest infections, sinusitis, avoid in tonsillitis
What is Flucloxacillin used for?
- skin and soft tissues infections e.g. cellulitis, osteomyelitis, infected eczema
What is Benzyl Penicillin used for?
- IM emergency treatment in suspected bacterial meningitis
What are the common uses for cephalosporins?
HAP- Hospital-acquired pneumonia
Biliary tree sepsis
Peritonitis
Meningitis
Septicaemia
10% sensitivity cross over with penicillins
WHat is PMAT and what does it do?
Plasma Membrane Monoamine Transporter
• Inhibit protein synthesis by binding to and interfering with ribosome
Examples of PMAT, common uses and side effects
- Macrolides- alternative to penicillins in patients with allergies e.g. for pneumonias and first line for atypical pneumonias
- enzyme inhibitors
- Gentamicin- gram negative anaerobes
- Nephrotoxic and ototoxic
- Doxycycline- malaria prophylaxis, acne, chlamydia
- Do not give to children- yellow teeth and bones
Examples of DNA replication blockers?
Metronidazole
Trimethoprim
Quinolones
WHat does Metronidazole and Trimethoprim do?
Metronidazole • Active against anaerobic organisms, often used in abdominal surgery, against protozoa, H pylori, dental infections
Trimethoprim - Inhibits the enzyme in bacteria which activates folate- therefore it cannot be given in pregnancy as folate is needed for neural tube formation- used for UTIs/ respiratory infections in non-pregnant adults
Examples of anticoagulants?
Warfarin - a vitamin K antagonist - affects factors 2, 7, 9 and 10
Heparin - binds to anti thrombin III and enhances its natural anticoagulant effect
Examples of enzyme inhibitors
think of O DEVICES
O- omeprazole
D- disulfiram
E- erythromycin
V- valproate
I- isoniazid
C- cimetidine + ciprofloxacin
E- ethanol (acute)
S- sulphonamides
Examples of enzyme inducers
think of PC BARS
P- phenytoin
C- carbamazepine
B- barbiturates
R- rifampicin
A- alcohol (chronic)
S- sulphonylureas
