Pharmacology Flashcards
Predicts the RATE of movement of molecules
Fick’s law of diffusion
Increase lipid solubility means increased absorption
True
Increased aqueous solubility means increased clearance
True
Pharmacokinetics is the?
Interaction of the body to the drug
Pharmacodynamics is the?
Interaction of the drug to the body
Relationshipd between ph and charge of molecule is predicted by?
Henderson-hasselbach equation
Which drugs are not given via IM due to the risk of causing hematomas?
Anticoagulants
Which route has partial bypass?
Rectal route cause the superior rectal vein absorptive n leads to bypass
Slowest route of drug administration
Topical route (local effect)
What route of administration undergoes first pass effect?
Oral route
Drug distribution is dependent on 4 factors which are?
Blood flow
Organ size
Protein binding
Solubility
Metabolic fate of the Drug?
A CITVATED
T ERMINATED
E LIMNATED
What Is the mode of elimination for drugs that are not metabolized?
Excretion
Rate of elimination is PROPORTIONATE to the CONCENTRATION
Rate of elimination decreases by 50% everytime
FIRST ORDER ELIMINNATION (most common)
Rate of elimination is CONSTANT regardless of concentration
Zero-order elimination
Concentration decreases linearly overtime
Zero-order elimination
What drugs display zero order kinetics?
WHAT PET (TOL BUTA ka naa sa sIDE o?)
Warfarin Heparin Aspirin Tolbutamide Phenytoin Ethanol Theophylline
Properties of a receptor
PMS
Most are PROTEINS
must be MODIFIED
must be SELCTIVE
_______ is the concentration required to bind 50% of the receptors
Kd
Smaller kd greater affinity
Concentration of a drug wherein half of the maximal effect is achieved
EC50
Maximal effect of a drug is defined by
EMAX
Maximal number of receptors bound are called
BMax
How do we compute for a THERAPEUTIC INDEX?
TI = TD50 / ED50
Higher TI the safer the drug
What is the therapeutic window?
It is the dose RANGE between the MEC and MTC
Drugs that display tachyphylaxis
MED Loves to watch CNN in HD
M etoclopramide
E phedrine
D obutamine
L SD
C alcitonin
N itroglycerin
N icotine
H ydralazine
D esmopressin
Most important pharmacokinetic parameter to be considered in defining a rational study state during dosage regimen
Clearance
Steady state is achieved in how many half lives?
4-5 half lives
Condition where administration is equal to elimination
Steady state
- amt of drug in the body does not change
What are phase I reActions?
HORDe
Hydrolysis
Oxidation
Reduction
Deamination
Drugs that are cytochrome P450 inducers
ETHel Booba takes PHEN-PHEN and Refuses Greasy Carb Shakes
Ethanol Barbiturates except secobarbital Phenytoin Phenobarbital Rifampicin Griseofulvin Carbamazepine Smoking and st.john's wort
Cytochrome p450 inhibitors
GRACE IS QVACK
Grapefruit juice Ritonavir Amiodarone Cimetidine Erythromycin
Isoniazid
Sulfonamides
Quinidine Valproic acid Allopurinol Chloramphenicol/chlorpromazine Ketoconazole
Suicide inhibitors
PASS
PTU
Allopurinol
Spironolactone
Secobarbital
Teratogenic effects
ACE INHIBITORS:\_\_\_\_\_\_\_\_\_\_\_ Antiepileptic drug:\_\_\_\_\_\_\_\_\_\_ Phenytoin:\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ OHA: \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_ Barbiturates:\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
ACE INHIBITORS: fetal renal damage Antiepileptic drug: neural tube defects Phenytoin: FETAL HYDANTOIN SYNDROME OHA: neonatal hypoglycemia Barbiturates: neonatal dependence
DIETHYLSTILBESTROL (DES) if given in a pregnant patient can cause?
VAGINAL CLEAR CELL ADENOCARCINOMA
Teratogenic effects
Ethanol:\_\_\_\_ Lithium:\_\_\_\_ Isotretinoin:\_\_\_\_\_ Iodide:\_\_\_\_\_\_\_ Misoprostol:\_\_\_\_\_\_
Ethanol: fetal alcohol syndrome Lithium: ebstein's anomaly Isotretinoin: caraniofacial malformations Iodide: congenital hypothyroidism Misoprostol: mobius sequence
Teratogenic effects
Penicillamine:\_\_\_\_\_ Thalidomide:\_\_\_\_\_\_ Streptomycin:\_\_\_\_\_ Methimazole:\_\_\_\_\_\_ Sulfonamide:\_\_\_\_\_\_ Flourquinolones:\_\_\_\_\_\_\_ Smoking:\_\_\_\_ Tetracycline:\_\_\_\_\_\_
Teratogenic effects
Penicillamine:cutis laxo Thalidomide: phocomelia Streptomycin: ototoxicity Methimazole: aplasia cutis congenita Sulfonamide: kernicterus Flourquinolones: cartilage damage Smoking:IUGR Tetracycline: tooth discoloration
Induction of changes in the genetic material
Mutagenesis
Induction of developmental defects in the somatic tissues
Teratogenesis
An ANS drug used as a miotic during ocular surgery
Acetylcholine
ANS DRUG used in Bladder and Bowel atony?
BETANECHOL
SE: Diarrhea and urinary urgency
ANS drug that increases aqueous humor outflow and increased salivation
Pilocarpine
Drug used for glaucoma, sjogren syndrome and sicca syndrome
Pilocarpine
SE: miosis, bov and increased salivation
Triad of sjogren syndrome
Xerostomia, xerophthalmia and rheumatoid arthritis
Dry
Drug used for smoking cessation activating autonomic post ganglionic neurons
Nicotine
Drug used to test Myasthenia Gravis in TENSILON TEST. It differentiates cholinergic crisis and myasthenic crisis.
EDROPHONIUM
DOA: 5-15 minutes
A cholinomimetic that is used to TREAT Myasthenia Gravis
NEOSTIGMINE
ALT : Pyridostigmine
Cholinomimetic drugs for ALZHEIMER’S DISEASE
Rivastigmine - available as a transdermal patch
Galantamine
Donepezil — combined with MEMANTINE (NMDA receptor blocker) for ALZHEIMER’S dementia
Signs and symptoms of ORGANOPHOSPHATE POISONING
DUMBBELSS
diarrhea urination miosis Bronchospasm Bradycardia Excitation of skeletal muscles and CNS Lacrimation Salivation Sweating
What do you give in a patient with organophosphate poisoning?
Atropine - antidote DOC
Notable SE: hyperthermia
Drug for organophosphate poisoning that should be given 6-8 hours after exposure to be rendered effective
PRALIDOXIME - antidote for early stage
This binds to phosphorus of organophosphate regenerating active acetylcholinesterase
Prototype nonselective muscarinic blocker
Atropine
Anticholinergics used for PARKINSON’S disease that reduces tremors
Muscarinic antagonists
Try Benz BEEP BEEP
trihexyphenidyl
Benztropine
BIPERIDEN
Ipratropium MOA
Its a muscarinic receptor antagonist that blocks receptors in bronchial smooth muscles preventing bronchoconstriction
USES: Acute asthma and COPD
Bronchodilator of choice for patients with COPD AND HEART DISEASE
Ipratropium bromide (less likely to cause arrhythmias and tachycardia)
Transdermal patch used for motion sickness
SCOPOLAMINE
SE: drowsiness, BOV, dry eyes, dry mouth, urinary retention and constipation
A muscarinic antagonist used in IBS
Dicyclomine / dicycloverine
A cholinergic antagonist used for urge incontinence by reducing detrusor muscle tone
Oxybutynin patch
Signs and symptoms of atropine toxicity
Hot as a hare (hyperthermia) Dry as a bone (decreased secretion) Red as a beet (cutaneous vasodilation) Blind as a bat (blurred vision) Mad as a hatter (CNS toxicity)
Contraindications to muscarinic blockers
ABCs of muscarinic receptor use
Acute angle closure glaucoma
Benign prostatic hyperplasia
Cautious use in infants
Only depolarizing neuromuscular blocker
Succinylcholine
DOC for anaphylaxis
Epinephrine
If epinephrine is given n a pregnant patient, the OB should watch out for?
Fetal anoxia
Given in neurogenic shock and the last resort for caridiogenic shock
Norepinephrine
Epinephrine can cause hyperglycemia or hypoglycemia?
Hyperglycemia
Toxic effects of norepinephrine
RATEE!
Reflex bradycardia Arrhythmias Tissue necrosis Excessive increase in BP Extreme vasospasm
Dose dependent action of dopamine
Low dose (1-5 mcg/kg/min) - D1 receptors increasing renal blood flow and urine output
Medium dose (5-15 mcg/kg/min) - B1 receptors increasing heart rate and contractility
High dose (>15 mcg/kg/min) - A receptors causing vasoconstriction thus increasing blood pressure
This is a synthetic catecholamine that is a beta nonselective sympathomimetic used in ASTHMA
Isoproterenol
An Alpha 1 selective sympathomimetic used for nasal decongestion
Phenylephrine
Notable SE: piloerction
Patient took 100 tablets of a sympathomimetic nasal decongestant. What can be given as antidote?
Phentolamine is the DOC for alpha 1 agonist overdose
Patient had rebound hypertension after abrupt withdrawal of clonidine. What can be given?
Phentolamine
An alpha 2 selective agonist given in opoid withdrawal?
Clonidine
*also given in cancer pain and hpn
Methyldopa is an alpha 2 agonist that is given in gestational hypertension and preeclampsia. What is a notable side effect of this drug?
Sedation and HEMOLYTIC ANEMIA (positive coomb’s test)
Alpa 2 agonist that decreases SECRETION of aqueous humor used in GLAUCOMA
Apraclonidine (C)
Brimonide (B)
SE: hyperemia, eye discomfort, pruritus,BOV and dry mouth
Beta 1 agonist used in cardiac stress testing
DOBUTAMINE
Drug of choice for acute asthma attack
Beta 2 selective agonist causing bronchodilation
Albuterol/ Salbutamol
Uses of ISOXUPRINE
Tocolysis for preterm labor
Vasodilator in Raynaud’s phenomenon
Beta 2 agonist drugs
S albutamol T erbutaline A lbuterol I soxuprine R itodrine
*TIR used for tocolysis
A sympathomimetic drug that causes appetite suppression and nasal vasoconstriction
Phenylpropanolamine
Tox: HEMORRHAGIC STROKE
An alpha nonselective antagonist used in the treatment of PHEOCROMOCYTOMA by IRREVERSIBLE blockage of alpha adrenergic receptors
PHENOXYBENZAMINE
An alpha nonselective antagonist used in the treatment of PHEOCROMOCYTOMA by REVERSIBLE blockage of alpha adrenergic receptors
Phentolamine, tolazoline
Uses of PHENTOLAMINE
Rebound hypertension
Antidote for alpha 1 agonist overdose
pheochromocytoma (presurgical)
Used for benign prostatic hyperplasia
Tamsulosin which is an alpha 1 selective antagonist that is most selective for prostatic smooth muscles
Other drugs: pazosin, terazosin “osin”
Pharmacologic advantage of a1 selectivity
Reflex tachycardia is less common and less severe
Beta blockers with intrinsic sympathomimetic activity
ISA PA
PINDOLOL
Acebutolol
Beta blocker with longest half life
NADOLOL =NAsa DOLO
Beta blocker with shortest half life
ESMOLOL = “esmol”
Beta blocker that treats Supraventricular tachycardia
Esmolol
Target BP of patients with no comorbidities
<140/90 JNC8
Target BP of patients with DM or CKD
<130/80
First line drug in a pregnant woman with hypertension
Methyldopa
2nd line treatment in a pregnant patient with hypertension
Labetalol
3 acceptable drugs that can be given in pregnancy for hpn control
Methydopa
Labetalol
Nifedipine
First line drug for hypertension
Thiazide diuretics
MOA of hyDroChloroThiazide
Inhibit Na/Cl transporter in Distal Collecting tubules causing diuresis
MOA of furosemide
This is a loop diuretic what inhibits NA/K/Cl transporter in thick ascending limb of loop of Henle
*can cause ototoxicity
Patient indicated for a loop diuretic with sulfa allergy. What can be given?
Ethacrynic acid
Diuretics can cause what acid base imbalance?
Hypokalemic metabolic alkalosis
Drugs used to control blood pressure in patients with PHEOCHROMOCYTOMA
Phenoxybenzamine
PHENTOLAMINE
Labetalol
Medications that may cause drug induced lupus
HIPP
Hydralazine
Isoniazid
Procainamide
Penicillamine
Treatment for alopecia
Minoxidil
Patient given a antihypertensive drug and developed pretibial edema. What drug could have been given?
Calcium channel blockers
benefits of ACE inhibitors and ARBs
HPN - decrease BP
Heart failure - slows ventricular remodeling and increases survival
Diabetic nephropathy - delays progression by decreasing albumin excretion
Most notable side effects of ACE inhibitors
Cough
Taste disturbance
Angioedema
Why do ARBs and ACE inhibitors cause hyperkalemia?
Decrease in aldosterone levels leads to potassium retention
Antidote for cyanide poisoning?
Lily cyanide kit
Inhaled AMYL NITRATE
IV SODIUM NITRITE
IV SODIUM THIOSULFATE
Why do patients taking nitrates complain of throbbing headache?
Due to meningeal blood vessel dilation
Drugs that cause gingival hyperplasia
NapaCa Pangit ng gingiVa mo
Nifedipine
Cyclosporine
Phenytoin
Verapramil
Drugs that are metabolism modifiers
Trimetazidne is fatty (beta oxidation)
Ranolazine is salty (na-ca rxchange)
Ivabradine is FUNNY (funny Na current in SA node)
Drugs with Narrow therapeutic index
WALA C Phen-phen VasTeD
Warfarin
Aminoglycosides
Lithium
Amphotericin B
Carbamazepine
Phenobarbital
Phenytoin
Vancomycin
Theophylline
Digixin
How do you treat digitalis toxicity?
Correct k and magnesium deficiency
Antiarrythmic drugs : DOC IS LIDOCAINE
Digoxin antibodies : digibind
First line of therapy for bith systolic and diastolic failure
FUROSEMIDE
What drugs have shown to improve survival in cases of heart failure?
ABS improve survival ;)
ACE INHIBITORS
BETA BLOCKERS
SPINOROLACTONE
What improves the quality of life?
Digitalis
Furosemide
Effects of class 1 antiarrythmics on action potential duration
Class 1a - “Ayyyee” = prolonges AP duration
Class 1b - “b” = shortens AP duration
Class 1c - no effect
Class IA antiarrythmics
Quinidine
Procainamide
Disopyramide
Class Ia antiarrythmic than can cause ITP AND TORASADES
Quinidine
Antidote for class IA antiarrythmics?
Sodium lactate
DOC for ventricular arrhythmias post MI
Lidocaine or any class I b antiarrythmics
Drugs that can cause agranulocytosis
CCCAPPIT Me!
Clozapine Co-trimoxazole Colchicine Amine pyrine Phenylbutazone PTU Indomethacin Tocainide Methimazole
Class I C antiarrythmics are contraindicated in?
POST MI PATIENTS WITH ARRHYTHMIAS
propafenone, flecainide, encainide
DOC antiarrythmics for WPW
Procainamide and amiodarone
Used for refractory arrthmias
Class IC
Propafenone
Flecainide
Encainide
Beta blocker with low lipid solubility
ATENOLOL
Beta blockers with Combined alpha and beta blockade
Carvedilol and labetalol
Beta blockers Lacking local anesthetic effect
Timolol
Beta blockers that are partial agonist
PINDOLOL AND ACEBUTOLOL
Antiarrythmics with a hallmark of prolongation of action potential duration
Class 3
Treatment and prophylaxis for atrial fibrillation
Class 3 antiarrythmics
DofeTILIde
IbuTILIde
Amiodarone toxicity signs and symptoms
Corneal deposits Skin deposits Thyroid dysfunction Pulmonary fibrosis Parestheisa Tremors
DOC for paroxysmal Supraventricular tachycardia
Adenosine
Major site for sodium chloride and sodium bicarbonate reabsorption
proximal convoluted tubules (60-70%)
Also site of uric acid transport and site of action of carbonic anhydrase
Site of action for calcium and magnesium reabsorption
Thick ascending loop of henle
Also site of loop diuretics
Loop diuretics toxicity
OH DANGS!
Ototoxicity
Hypokalemia
Dehydration Alkalosis Nephritis Gout Sulfa allergy
Side effects of thiazide diuretics
Hyper GLUC
HYPERGLYCEMIA
HYPERLIPIDEMIA
HYPERURICEMIA
HYPERCALCEMIA
Site of action of thiazide diuretics?
Distal convoluted tubules
Site of action for potassium sparing diuretic
Cortical collecting duct
-last tubular site for sodium reabsorption and potassium excretion
Primary site for urine acidification
Cortical collecting duct
Drugs that can cause gynecomastia
DACKS
Digoxin Alcohol Cimetidine Ketoconazole Spironolactone
Site of action of mannitol
Osmotic diuretics act on the proximal tubule, descending limb of loop of Henle and collecting ducts
Site of action of ADH agonist
Vasopressin acts on the collecting tubule
DOC for lowering LDL cholesterol
Statins
DOC for high triglycerides and VLDL
Fibrates
EZETEMIBE +STATIN =?
Hepatotoxicity
STATIN + FIBRATES =?
rhabdomyolysis
If statins are to be given with resins how will the drugs be taken?
Statins should be given one hour before or 4 hours after resin intake
Why are statins given in patients with CAD?
For stabilization of atherosclerotic plaques
Fibrates + Bile resins =
Cholesterol stones
CI in cholestyramine
Patients with HIGH TG and Diverticulitis
Common SE of bile acid resins like cholestyramine
CONSTIPATION
BLOATING
GRITTY TASTE
STEATORRHEA
Most effective drug to increase HDL levels
NIACIN
Drugs that causes FLUSHING
VANC
Vancomycin
Adenosine
Niacin
Calcium channel blockers
When giving NIACIN what can be given as pre treatment to avoid flushing?
ASPIRIN
Endogenous molecules with powerful pharmacologic effects
Autacoids
Histamine and serotonin are important amine autacoids
Triple response of Lewis
Wheal flush and flare
Cimetidine notable side effects
Gynecomastia and CYP450 inhibitor
Decrease hepatic blood flow
Drug of choice for ACUTE MIGRANE
Sumatriptan-5Ht1D agonist
NSE: coronary vasospasm and chest pain
Indication for Ondansteron given in cancer patients and post surgery patients
For chemotherapy and post operative vomiting
5HT3 antagonist
Indications for MISOPROSTOL
NSAID INDUCED BPUD and Abortifacient
Indications for use of ALPROSTADIL
For maintenance of a PDA
For ERECTILE DYSUNCTION (injected in the cavernosa)
A Prostaglandin E2 analog given for induction of labor and cervical ripening
Dinoprostone / Sulprostone
A Prostaglandin F2 analog that is given for postpartum bleeding
BUTCH
BIMATORPOST
UNOPROSTONE
TRAVOPROST
CARBOPROST
Prostaglandin I2 analog that reduces platelet aggregation in dialysis machines and for pulmonary hypertension
Epoprostenol
Prostaglandin F2 analog sed to increase outflow of aqueous humor in glaucoma
Latanoprost
SE: change eye color
Indications for SILDENAFIL, a PDE5 inhibitor
PRE!
Pulmonary arterial hypertension
Reynaud’s phenomenon
Erectile dysfunction
Doc in acute asthma attacks
SABA - PAST
Procaterol
Albuterol
Salbutamol
Terbutaline
DOC in asthma prohylaxis
Corticosteroids
Fluticasone
Mometasone
Budesonide
Beclomethasone
Muscarinic antagonist used in ACUTE ASTHMA AND COPD
Ipratropium
Prophylactic against NOCTURNAL ASTHMA ATTACKS
Aminophyline and theophylline
Antidote for overdose of theophylline
Beta blockers
Mast cell stabilizer for asthma prophylaxis and ophthalmic allergies
Cromolyn
DOC for prophylaxis of severe , refractory asthma not responsive to all other drugs
Omalizumab - anti IgE antibody
Iron supplement with greatest iron content
Ferrous fumarate
Chronic Iron overdose may lead to?
Hemochromatosis-> organ failure ->death
Acute Iron intoxication can be chelated by?
DEFEROXAMINE
*intox common in children from accidental ingestion
Hemochromatosis triad
CIRRHOISIS
DIABETES MELLITUS
SKIN PIGMENTATION
Neurologic manifestations of vitamin B12 deficiency
Ataxia
Impaired position and vibratory sense
Spasticity
Toxic dose of ASA? Lethal dose?
Toxic at 150mg/kg
Lethal at 500mg/kg
Triad for ASPIRIN HYPERSENSITIVITY
SAMTER TRIAD
asthma
Aspirin sensitivity
Nasal polyps
What is the expected metabolic abnormality in salicylate poisoning?
RESPIRATORY ALKALOSIS WITH HIGH ANION GAP METABOLIC ACIDOSIS (HAGMA)
Difference between adults and children in presentation of ASA intoxication
Adults = mixed acid base disorder (respi alka with HAGMA)
Children= will have HAGMA purely
A GIIa/IIIa inhibitor used during PCI and adjunct to thrombolysis. This also prevents VESSEL RESTENOSIS AND REINFARCTION
Abciximab
Heparin
Site of axn? Route? MOA? Monitoring? Antidote?
Site of axn? Blood Route? Parenteral MOA? Activates ANTITHROMBIN III Monitoring? PTT Antidote? PROTAMINE
Warfarin
Site of axn? Route? MOA? Monitoring? Antidote?
Site of axn? LIVER Route? ORAL MOA? impairs post-translational modifications of FACTORS 2,7,9,10 Monitoring? PT Antidote? Vitamin K , FFP
Lab tests to assess the extrinsic and intrinsic coagulation pathways
PiTT and PeT
PiTT for intrinsic
PeT for extrinsic
DOC for anticoagulation in pregnancy
Heparin
Anticoagulant of choice for patients with HEPARIN-INDUCED THROMBOCYTOPENIA
Lepirudin
Argatroban
Desirudin
DABIGATRAN (po)
Given for DABIGATRAN toxicity
IDARUCIZUMAB
MOA of APixaban / Rovaroxaban
Oral direct factor Xa inhibitor in the final common pathway
Use: prevention of VTE and stroke in AF
This drug inhibits VIT K EPOXIDE REDUCTASE and is used for chronic anticoagulation
WARFARIN
NSE: warfarin induced skin necrosis for pts with protein C and S deficiency
Initial anticoagulatant of choice in patient management?
Heparin
Antidote for overdose of THROMBOLYTIC AGENTS such as streptokinase, urokinase and alteplase
AMINOCAPROIC ACID
A drug that can increase factor VIII activity of patients with vonWillebrand disease
Desmopressin / vasopressin
What are the features of tricyclic antidepressant overdose?
3 Cs of TCA
coma
Convulsions
Cardiotoxicity
Symptoms of SEROTONIN syndrome
FAT CHD
Fever Agitation Tremors Clonus Hyperreflexia Diaphoresis
Triad of OPIOD overdose
PCR
Pupillary constriction
Comatose state
Respiratory depression
What drug of abuse can lead to a dream-like state, RED conjunctiva, tachycardia and dry mouth?
Marijuana
What drug of abuse can cause psychedelic effects, mind raveling effects and bad trips?
LSD
Most dangerous hallucinogen with psychomimetic effects
Phencyclidine
Ecstasy can cause?
Sexual enhancement and hyponatremia
Amphetamine can cause?
Euphoria, sleeplessness and self confidence
Can cause crack lung and mydriasis
Cocaine
Patient receiving cyclophosphamide should also be given
MESNA
Patient given with methotrexate should also be given
Leucoverin
Patients given with isoniazid should also be given
Pyridoxine
Alcoholics should take _____ as supplements
Thiamine
Dissociative amnesia is effectively achieved by combination of
Ketamine
Nitrous oxide
Fentanyl