PHARMA PEARLS Flashcards
Refers to the amount of a drug that reaches the systemic circulation
BIOAVAILABILITY
Used to determine the safety and efficacy of generic drugs
BIOEQUIVALENCE
Measure the dose or concentration required to bring about 50% of the drug’s maximal effect
POTENCY
Dose at which 50% of individuals exhibit the specified quantal effect
MEDIAN EFFECTIVE DOSE
Dose at which 50% of the animals manifest a particular toxic effect
MEDIAN TOXIC DOSE
Transfer of drug from site of administration to bloodstream
ABSORPTION
Refers to the apparent volume into which the drug is able to distribute
VOLUME OF DISTRIBUTION
Elimination of a drug at a constant rate (Irrespective of Concentration)
ZERO-ORDER KINETICS
Elimination at a rate that is proportional to the serum concentration of the drug
FIRST-ORDER KINETICS
Addition of a polar moiety (Sulfate, Acetate or Glucoronate)
PHASE II METABOLISM
Use of CYP450 system oxidation, reduction or hydrolysis
PHASE I METABOLISM
Describes the rate at which a specific drug is cleared from the system
CLEARANCE
Refers to the amount of time required for the amount of drug in the body to decrease the half of its value after the administration of the drug has been stopped
HALF-LIFE
Defined as the single amount of drug that is needed to achieve a desired plasma concentration quickly
LOADING DOSE
Amount of drug that must be given over time in order to maintain desired plasma concentration
MAINTENANCE DOSE
Used as a measure of drugs safety
THERAPEUTIC DOSE
Formula for therapeutic index
TD50/ED50 (TD: Toxic Dose, ED: Effective Dose)
Refers to the dosage range between the minimum effective therapeutic concentration or dose and minimum toxic concentration or dose
THERAPEUTIC WINDOW
Substance that shifts the graded dose-response curve to the right
COMPETITIVE ANTAGONIST
Substance that does not produce the same maximum effect and is exhibited by a decrease in Emax
IRREVERSIBLE ANTAGONIST
An antagonist that interacts directly with the agonist and not at all or only incidentally with the receptor
CHEMICAL ANTAGONIST
The action of the drug on the body
PharmacoDynaMics
The action of the body on the drug
PharmacoKineTics
Permeation that is governed by Fick’s Law
AQUEOUS DIFFUSION
Permeation that is saturable and inhibitable
CARRIER TRANSPORT
Adverse effect that is infrequently observed in most patients
IDIOSYNCRATIC
Responsiveness decreases as a consequence of continued drug administration
TOLERANCE
Responsiveness diminishes rapidly after drug administration
TACHYPHYLAXIS
Induction of developmental defects in the fetus
TERATOGENESIS
Induction of malignant characteristics in cells
CARCINO- GENESIS
Induction of changes in the genetic material of animals of any age
MUTAGENESIS
Cytochrome P450 Inducers
(ETHel Booba takes PHEN-phen and Refuses GReasy CARB Shakes): Ethanol, Barbiturates, Phenytoin, Rifampicin, Griseofulvin, Carbamazepine, St. John’s Wort/ Smoking
Cytochrome P450 Inhibitors
(Inhibitors Stop Cyber Kids from Eating GRApefruit QV): Isoniazid, Sulfonamides, Cimetidine, Ketoconazole, Erythromycin, Grapefruit Juice, Ritonavir, Amiodarone, Quinidine, Valproic Acid
100% bioavailability
INTRAVENOUS
First Pass Effect
ORAL
Partial Avoidance of First Pass Effect
RECTAL
Application to skin for local effect
TOPICAL
Application to skin for systemic effect
TRANSDERMAL
Small number of normal volunteers; Determines if drug is Safe
PHASE 1
Post-Marketing Surveillance; Drug Approved for Circulation; Watching out for Side Effects/ Adverse Effects of the Drug
PHASE 4
“Does it work on patients?”; 20-100 subjects
PHASE 2
Randomized double-blind, controlled trials; “Does the drug benefit the intended subjects?”
PHASE 3
A drug for a rare disease
ORPHAN DRUG
What agent used to hasten excretion in a Weak Base Overdose (Diphenhydramine)
ACIDIFYING AGENT (AMMONIUM CHLORIDE)
What agent used to hasten excretion in a Weak Acid Overdose (Aspirin)
ALKALINIZING AGENT (SODIUM BICARBONATE)
Vasoconstriction via Alpha 1 Receptors in Smooth Muscles
EPINEPHRINE > NOREPINEPHRINE
Inhibit Release of Neurotransmitters via Alpha 2 Receptors in Nerve Terminals
EPINEPHRINE > NOREPINEPHRINE
Increase Rate and Contractility via Beta 1 Receptors in the Heart
ISOPROTERENOL > EPINEPHRINE > NOREPINEPHRINE
Broncho/ Vasodilation via Beta 2 Receptors in Respiratory Smooth Muscles and Uterus
ISOPROTERENOL > EPINEPHRINE > NOREPINEPHRINE
Vasodilation of Renal Blood Vessels via D1 Receptors in Splanchic and Renal Vessels
DOPAMINE
Regulate Neurotransmitters via D2 Receptors in Nerve Terminals of CNS
DOPAMINE
Bowel and Bladder Atony
BETHANECOL (Direct Acting Muscarinic Agonist at M2-M3)
Sjogren Syndrome (Xerostomia, Xerophthalmia & Rheumatoid Arthritis)
PILOCARPINE (Direct Acting Muscarinic at M1, M2, M3)
Diagnosis of Myasthenia Gravis, Differentiation of Myasthenic and Cholinergic Crisis)
EDROPHONIUM (Indirect Acting Cholinomimetic) MOA: Hydrolysis of Cholinesterase
Treatment of Myasthenia Gravis
NEOSTIGMINE
Reversal of Nondepolarizing Neuromuscular Block
NEOSTIGMINE
Treatment of Glaucoma (Cholinergic Drug)
PHYSOSTIGMINE
Diagnosis of Bronchial Hyperreactivity
METHACOLINE (Direct Acting Cholinomimetic)
Treatment of Alzheimer’s Disease
DONEPEZIL (Reversible Acetylcholinesterase Inhibitor)
Bowel and Bladder Atony
BETHANECOL
Autoimmune disorder characterized by triad of 1. Xerostomia (Dry Mouth) 2. Xerophthalmia (Dry Eyes) 3. Rheumatoid Arthritis
SJOGREN SYNDROME
Autoimmune destruction of nicotinic acetylcholine receptors characterized by fluctuating muscle weakness: 1. ocular symptoms 2. bulbar symptoms 3. proximal muscle weakness
MYASTHENIA GRAVIS
Acute worsening of symptoms due to infection, stress or UNDERmedication
MYASTHENIC CRISIS
Excessive activation of cholinoreceptors (skeletal muscle weakness and parasympathetic signs) due to OVERmedication
CHOLINERGIC CRISIS
Differentiate MYASTHENIC CRISIS from CHOLINERGIC CRISIS using EDROPHONIUM
EDROPHONIUM IMPROVES muscle strength in MYASTHENIC CRISIS while it WEAKENS muscle strength in CHOLINERGIC CRISIS
Small Cell Cancer presenting with a Myasthenia-like Paraneoplastic Syndrome
LAMBERT-EATON SYNDROME (Destruction of Presynaptic Voltage-Gated Calcium Channels by Antibodies)
What are signs and symptoms of Organophosphate Poisoning
DUMBBELSS: Diarrhea, Urination, Miosis, Bronchospasm, Bradycardia, Excitation (Skeletal Muscles and CNS), Lacrimation, Sweating, Salivation
Induction of Mydriasis and Cyclopegia
TROPICAMIDE
Sinus Bradycardia
ATROPINE
Cholinergic Antagonist used as 2nd Line Treatment for Parkinson’s Disease; Improves tremors
BENZTROPINE
Cholinergic Antagonist for COPD
IPRATROPIUM (M3 Antagonist)
Motion Sickness, Sea Sickness
SCOPOLAMINE
Gastrointestinal Spasms
HYOSCYAMINE
Treatment for Organophosphate Poisoning/ Nerve Gas Poisoning
ATROPINE (Reverses effect of Acetylcholine esp Muscarinic Effects) & PRALIDOXIME (given first; 6-8 hours effect duration)
Muscarinic Antagonists for Parkinson’s Disease
TRI to park your BENZ, BIP here: TRIhexyphenidyl, BENZtropine, BIPeriden
Why is Ipratropium the preferred bronchodilator in patients with comorbid COPD and Heart Disease?
IPRATROPIUM less likely to cause tachycardia and cardiac arrhythmias
Signs of Atropine Toxicity
HOT as a hare, DRY as a bone, RED as a beet, BLIND as a bat, MAD as a hatter; CI: Infants, BPH, Acute-Angle Closure Glaucoma
DOC for Anaphylactic Shock, Adjunct to local anesthesia, Cardiac Arrest, Croup
EPINEPHRINE (Equal affinity to Alpha & Beta Receptors; Acts like a HORMONE)
Acute CHF, Cadiac Stress Testing
DOBUTAMINE (β1)
Acute CHF, Shock (Cardiogenic, Septic)
DOPAMINE
Drug of Last Resort for Shock
NOREPINEPHRINE (α1, α2, β1); Acts like a Neurotransmitter
Nasal Congestion, Mydriasis WITHOUT Cycloplegia
PHYNELEPHRINE
SE: Rebound Hypertension on Discontinuation
CLONIDINE
SE: Hemolytic Anemia (Positive Coomb’s Test)
METHYLDOPA (Centrally Acting for Preeclampsia)
Bronchial Asthma, COPD
SALBUTAMOL (Selective β2-agonist)
Tocolysis for Preterm Labor
TERBUTALINE
You have 1 HEART and 2 LUNGS
β1 for HEART, β2 for LUNGS
Preoperative treatment of Pheochromocytoma
PHENOXY- BENZAMINE (Irreversible Nonselective; for UNRESECTABLE tumor)
Treatment of Rebound Hypertension in Pheochromocytoma
PHENTOLAMINE