Neuro drugs
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Transcript of Neuro drugs
DRUGS CHEAT SHEET
CARDIO
CLASS GENERAL/TRADE NAME
MECHANISM INDICATIONS SIDE EFFECTS/DRUG INTERACTIONS/PRECAUTIONS
ANTI-HYPERTENSIVEβ-Blocker (β-Blocker for the LOLs)
Propanolol (Non-selective)
Atenolol (Selective)
Metoprolol
Block B1-adrenegic receptor Decrease sympathetic activity Decrease intracellular cAMP Muscle relaxation REDUCE INOTROPY
First line prescription for myocardial infarction
Contraindications:- Asthmatic patients
Side effects:- Bronchoconstriction - Increase risk of
diabetes - Peripheral vascular
disease/cold extremities
- Mask hypoglycaemia (atenolol preferred)
- Nightmares/dreams (propranolol)
- Heart block in combination with verapamil
Ca2+ channel blocker Verapamil Diltiazem
Heart:Block Ca2+ channel No influx of extracellular calcium No calcium release from SR Reduce contractility REDUCE INOTROPY & CHRONOTROPY
Peripherals:Decrease Ca2+ influx in peripheral smooth muscles Vasodilation
- ACEI+CCB - diabetes
- Beta blocker + dihydropyridine - CHF
Contraindications:- Patients on B-blocker
cannot be prescribed with verapamil
- Negative inotropy drugnot to be used in heat failure!
Side effects:- Flushing and peripheral
oedema (dihydropyridines)
- Heart block/heart failure
(verapamil/diltiazem) A2RA (Angiotensin 2 receptor antagonist)
Losartan Valsartan
Block angiotensin 2 receptor in RAAS:
- Decrease BV - Decrease BP
*refer to ACE inhibitor below
Prescribed to patients with coughing with ACE-inhibitor use
- Headache, dizziness- Rashes- Angio oedema- Photosensitivity- Hyperkalaemia
(aldosterone inhibition)- Hypotension (on first
dose)ACE inhibitor Trandolapril
Captopril- Stop RAAS (refer to
diagram below)- Inhibit the
conversion of bradykinin to inactive bradykinin Vasodilation Decrease TPR Decrease afterload Decrease cardiac workload (CO) Decrease BP
First line prescription in:- Myocardial
infarction- Hypertension- Heart failure- <65 years old
( Lack of diabetes)
- Diabetes with proteinuria
- Coughing- Rash/angioedema - Hyperkalaemia - First-dose hypotension- Headache, dizziness,
fatigue, nausea.
Diuretics Loop diuretics Furosemide
- Acts on Na/K/2Cl cotransporter at Loop of Henley
- Inhibit the reuptake of Na from tubule
- Water follow salt
- Hypokalaemia
Thiazide (Metalazone, caffeine)
- Acts on Na/Cl at distal convotuled tubule
- Hypokalaemia
K-sparing Spironolactone/
Aldectone
- Inhibit Na/K antiport at cortical collecting tubule
Aldactone:
- Hyperkalaemia
- Inhibit aldosteroneANTI-PLATELETS
Aspirin - Inhibit COX1 pathway irreversibly
- Reduce thromboxane A2
- Also reduce prostacyclin which inhibit platelet aggregation but the production of TXA2 takes longer time to recover and thus, the anti-platelet effects of aspirin outweigh this effect.
- Arrhythmia- Heart and valve
replacement surgery
Contraindications:- Pregnancy
Side effects: Always give together
clopidogrel/dipyridamole
Bleeding Asthma
Warfarin Vitamin K antagonist inhibit reduction of vitamin K (reduction as in reduce dlm REDox) inhibit activation of clotting factors (2, 7, 9, 10)
- Blood coagulation problems (DVT, PE)
- Atherosclerosis/ MI
- Stroke- Atrial fibrillation - Refer to
indication for aspirin
Contraindications: - Pregnancy
Side effetcs:- Bleeding &
haemorrhage- Warfarin necrosis in
patients with protein C deficiency (thrombosis with skin necrosis and gangrene)
- OsteoporosisCHOLESTEROL CONTROL
Statin HMG-CoA reductase inhibitor
Lipitor Simvastatin
HMG-CoA reductase inhibitorreduction in mevanolate levels. Normal mechanism; HMG-CoAmevanolate
- High risk for hypercholesterolaemia (family history, weight, age)
Side effects- Hepatic damage- Myalgia- Myopathy - Muscle cramps
(by the action of HMG-CoA reductase)cholesterol
Fibrates PPar-alpha receptor agonistincrease beta oxidation in the liver (beta oxidation converts fatty acidacetyl-CoA)lower fatty acidAlso; PPar-alpha receptor agonist increase lipoprotein lipase(1) increase breakdown of LDL, (2) increase breakdown of triglyceride, (3) increase reuptake of LDL (reuptake of LDLdecrease LDL in blood)
Side effects- GI disturbance- Myopathy (increase
when taken with statin)- Cholestatic jaundice- Gallstone formation
Ezetimibe Decrease absorption of cholesterol from duodenum (does not affect triglyceride and fat soluble vitamin)
Also; increase hepatic uptake of LDL decrease of LDL in blood
Side effects- Steatorrhoea - Fatigue- Headache - Hepatitis - Raised LFT- Myalgia - Rashes- Myopathy
ANTI-ARRHYTHMIA
I Na+ channel blocker Quinidine (prokinamide, disopyramide)
Indications:- Ventricular arrhythmia - WPW (just
prokinamide)- Recurrent AF
*kene letak sini sbb diagram besaq sangat
IIβ-blocker Propanolol Atenolol
Bind to B-receptor in cellinhibit sympathetic
- Refer to atas aku dah malas dah
Side effects pun same paham paham je la
Metoprolol actionreduce firing rate of SA nodereduce heart rate
nk type ni woi
IIIK+ channel blocker Amiodarone Dronedarone
Hyperpolarisation prolongs QT interval
- Tachycardia without sinus rhythm
- VT/VF in acute MI
Side effects:- Torsade des pointes
IVCa2+ channel blocker
Verapamil Diltiazem
Block voltage-sensitive calcium channel (L-type calcium channel)inhibit Ca2+ entry caused by depolarizationslows down AP conduction from SA to AVslows down HR
- Reentrant SVT- PSVT- AF
Precautions:- NEVER EVER GIVE to
people with VT!- If given via
IVhypotensionSide effect:
- Heart block V Adenosine, Digitalis, Magnesium
Adenosine Cause hyperpolarisation more time needed to reach threshold (1) slows HR, (2) regulate the firing of SA node, (3)slows down conduction through AV node
Also; decrease cAMPdecrease in inward pacemaker current and the inward calcium currentslows down SA firing rate and also AV node conductionslows HR
- Torsade des pointes
- SVT- PSVT- Reentrant SVT
Side effects:- Confusion - Headache- Bronchoconstrriction- Flushing
Digitalis Enhance vagal tone decrease sympathetic decrease frequency of transmission between SA
Supraventricular reentrant arrhythmia
Contraindications:- Not to be given to pt
with renal failure Side effects:
Node and AV node increase refractory period in AV node reduces ventricular rate
- Nausea- Vomiting- Arrhythmia- Confusion- Toxic effects: digitalis
induced arrhythmia through (1) less –ve resting potential, (2) decrease action potential duration, (3) entrance automaticity
Magnesium Nil Digitalis induced arrhythmia patients
Nil
POSITIVE INOTROPIC Cardiac glycosides Digitalis
(Digoxin)Inhibition of Na+/K+ exchange channel increase Na+ in myocytes decrease Na+/Ca2+ exchange via Na+/Ca2+
antiport increase Ca2+ increase inotropy/contractility
Ditto
Sympathomimetics Catecholamine (adrenaline, noradrenaline, dopamine)
Dobutamine PDE-3 inhibitor (phosphodiaterase-3 inhibitor)
Enoximoxone
ANALGESICOpiods Morphine
(Loperamide)Bind to opioid receptors at CNS block ascending pathway of perception block pain perception
Given to patients with angina when pain not improved with nitrates
Opioid also present in GI system and thus, drugs may cause GI disturbance
VASODILATOR
Organic nitrates GTN (under-the-tongue nitrate/ sublingual)
Anginine
GTN denitrated into NO (active metabolite that causes vasodilation) GTP is converted into cGMP cause muscle relaxation
Given sublingually as to escape first pass metabolism
- Unstable angina
PDE -5 inhibitor (phosphodiaterase-5 inhibitor)
Sildenafil Inihibit cGMP breakdown in cells relaxation enhance vasodilation and oxygenation
Ca2+ channel blocker Dihydropyridine (amlodipine, felodipine)
Peripherals:Decrease Ca2+ influx in peripheral smooth muscles Vasodilation
RAAS
ANGIOTENSIN 1
THIRST
ANGIOTENSINOGEN
VASOCONSTRICTION
ACE
ANGIOTENSIN 2
RENIN
ALDOSTERONE ADH SNS (INC.)
Released when:
Reduced renal perfusion, decrease CO2, increase sympathetic
Inhibit by ACE INHIBITOR
Released by lungs and kidneys
RESPI
CLASS GENERAL/TRADE NAME MECHANISM INDICATIONS SIDE EFFECTS/DRUG INTERACTIONS/PRECAUTIONS
BRONCHODILATORS
Beta-agonists - Short acting B-agonist (Salbutamol, Terbutalin)
- Long acting B-agonist (Salmeterol, Formoterol)
B-agonist bind to B-receptor increase in CAMP increase in intracellular PKA phosphorylation of myosin light chain kinase inhibit muscle contraction
Increase mucus clearance (mechanism unknown)
- Asthma (SABA & LABA)
- COPD (LABA)
Contraindications:
- Patients with cardiovascular disease
Side effects:
- Tremors (due to stimulation of peripheral smooth muscle)
- Tachycardia
- Tolerance
- anxiety
Muscarinic receptor anatgonist
- Short acting (Ipratropium bromide)
Normal fx:
Acetylcholine bind to M3 receptor Activate phospholipase C Increase in IP3 Increase in intracellular CA2+ muscle contraction
*block Ach from binding to M3
- Asthma - Dry mouth
- Throat irritation
receptors
- Long acting (Tiotropium bromide)
Dissociate from M1 to M3 more slowly than M2.
- COPD
Leukotriene antagonist
Zafirlucast, Montelukast Blocks the conversion of leukotriene C4 to leukotriene D4 Decrease in concentration of leukotriene D4 Decrease in inflammation
- Add on therapy to inhaled corticosteroid when LABA is not tolerated
- For frequent intermittent asthma, aspirin-induced and eosinophilic asthma
Methylxanthine Theophylline Normal fx:
Inhibit
ATP CAMP AMP
Thiophylline: Inhibit the conversion of CAMP to AMP increase in CAMP muscle relaxation
ANTI-INFLAMMATORY
Corticosteroids Inhaled: Glucocorticoids: - Asthmatic pt Inhaled:
Fluticasone, Budesonide, Beclomethosone
Oral:
Prednisolone
Bind to the glucocortocoid promoting elements (GRE) in the promoter region of the specific gene to alter the gene production of protein that inhibit inflammation (lipocortin) block arachidonic acid pathway at membrane phospholipid reduce inflammation.
- COPD pt - Voice change
Oral:
- Cushing’s syndrome
- Weight gain
- Puffy face
- Hypertension
- Glaucoma
- Cataract
Cromones Chromoglycate, Nedocromil Inhibit mast cells degranulation inhibit the release of histamine
*Mechanism is not fully understood
- Any airway inflammatory disease
ANTIBIOTICS
Cell wall synthesis inhibitor
B-lactams (Penicillin, Vancomycin)
- Bactericidal
Interfere with the sysnthesis of the bacterial cell wall inhibit the transpeptidases that cross-link the peptide chains attached to the backbone of the peptidoglycan weaken the cell wall leads to bacterial lysis bacterial death
Tolerance:
Normal: Penicillin binds to
- Pneumonia
- Vancomycin is used for patients who are resistant to penicillin (because it is a glycopeptides antibiotic and not a B-lactam)
- Metronidazole is used for patients
Contraindications:
- Allergy/ hypersensitivity
bacterial cell wall inactivation of inhibition of autolytic enzyme lysis of cell wall
Abnormal:
- Inactivation by B-lactamase production of B-lactamase is the major mechanism of resistance to the B-lactam B-lactamase cleaves predominantly penicillin, cephalosporins or both production may be encoded within the bacterial chromosome / gene may be acquired on plasmids or transposon
- Defective autolytic enzyme Bacteria is not lysed even in the presence of drugs
- Alteration of active site of target receptor in bacterial cell wall Unable to bind
who are allergic to B-lactams
- Decrease penetration to the target site gram negative provides good barrier to the penetration of B-lactams antibiotics to the target PBP (Penicillin binding protein) Usually must pass through hydrophilic protein channels in the outer membrane of the gram negative bacilli to reach periplasmic space
DNA synthesis inhibitor
Folate affectors (sulfonamides)
Disrupt folic acid synthesis:
Protein synthesis Macrolides (Erythromycin, Clarithromycin,
Block 50s subunit of ribosome which then inhibit bacterial
- Hypersensitivity
inhibitor azithromycin) protein synthesis - Rashes
- GI disturbance
- Fungal growth
- Fever
Tetracyclines Block 30s subunit of ribosomes which inhibit bacterial protein
- Dizziness
- GI distress
- Photosensitivity
- Skin and mucus pigmentation
- Oral, rectal and genital fungal growth
Topoisomerase inhibitor
TAK FOFULER Disrupt gene transcription by affecting the unfolding process
Anti protozoal drugs Metronidazole Active against anaerobic bacteria and amoebas organisms will reduce metronidazole to its active form intracellulary reduced drug then binds to DNA causingstrand breakage, dissolution of helix formation and overall degradation of the DNA
For those allergic to penicillin
EMERGENCY
Analgesics - ABCDEF management of pneumonia
- COPD
Anti- Biotics Penicillin
CPAP Positive pressure oxygen via nasal prongs
- Blue bloaters is contraindicated for 100% O2 monitor patient’s consciousness discontinued and put on 21% oxygen via mask
Drain Draining fluid in pulmonary oedema
- Physiotherapist
- Diuretics
Extra air Increase O2
Fluid Intravenous fluid Dehydration decrease BP to restore/ maintain BP
ANTI-MUCOLYTIC
Mucolytic agent Acetylcysteine Mechanism is not fully understood
- Any disease with hypersecretion
- Asthma
- COPD
HAEM
CLASS GENERAL/TRADE NAME MECHANISM INDICATIONS SIDE EFFECTS/DRUG INTERACTIONS/PRECAUTIONS
DNA DAMAGING
Alkylating agents - It interferes with DNA synthesis by breaking the cross-link of the DNA strands.
- It affects the cross-link by covalently binding alkyl groups to DNA strands.
Anti-metabolites - Pyrimidine antagonist
- Purine antagonist
- Arabinosides
- Inhibit nucleic acid synthesis
Folic acid antagonist Refer kat atas
DNA REPAIR INHIBITORS
Epipodophyllotoxins Topoisomerase inhibitor
It can inhibit either:- Topoisomerase I:
irinotecan & topotecan - Topoisomerase II:
etoposide
Topoisomerase I:
- Used in lung, colon, ovary and cervix cancer
Topoisomerase II:
- Used in wide range of cancers
Cytotoxic antibiotics - Intercalate adjoining - Used in
nucleotide pairs in the same DNA strands
- Inihibit topoisomerase II DNA repair
haemotological and solid cancer
ANTI-TUBULIN
Vinca alkaloids - Bind to tubulin microtubule formation
- Must never be given intratecally (into spinal theca)
- Associated with neurotoxicity due to their anti-microtubule effect
Taxanes - Bind to tubulin dimmers prevent assembly into microtubules
- Used in many cancers including ovarian, breast and lung cancer
Patients should be premedicated with steroids, H1 and H2 histamine antagonists prior to treatmen
Can cause neurotoxicity and hypersensitivity reactions