PHARMA LEC 1 Flashcards
Which of the following drugs follow zero-order kinetics? Select one or more
A. Ethanol
B. Gentamycin
C. Phenytoin
D. Aspirin
A. Ethanol
C. Phenytoin
D. Aspirin
Most drugs have molecular weights between 100-1000. This lower limit prevents drug from
A. being premature cleared from circulation
B. dissociating until it reaches the target organ
C. binding to other receptors
D. moving from one body compartment to another
C. binding to other receptors
A drug X is said to achieve maximal efficacy when:(select one or more)
A. no increase in response happens when a higher concentration of drug is obtained
B. repeated administration of drug X results to downregulation of receptors
C. affinity exceeds saturation for drug X
D. all physiologic receptors for drug X are full saturated
A. no increase in response happens when a higher concentration of drug is obtained
D. all physiologic receptors for drug X are full saturated
Which of the following statements correctly differentiates irreversible antagonism from allosteric antagonism? The latter
A. binds to a site other than the agonist-binding site
B. cannot be overcome by adding more agonists
C. causes a downward shift of the Emax
D. shifts the agonist-dose response curve to the right
A. binds to a site other than the agonist-binding site
Which of the following phase II metabolic reactions makes phase I metabolites readily excretable in urine?
A. Reduction
B. Hydrolysis
C. Glucuronidation
D. Oxidation
C. Glucuronidation
What is the most important parameter to consider when designing a regimen for a long-term duration of administration?
A. Half-life
B. Volume of distribution
C. Clearance
D. Bioavailability
C. Clearance
Which of the following route of drug administration reduces hepatic first-pass loss by more than 50%? Select one or more
A. Rectal
B. Inhalation
C. Transdermal
D. Sublingual
B. Inhalation
C. Transdermal
D. Sublingual
Which of the following factors would provide the greatest influence on absorption via the enteral route?
A. Drug concentration
B. Gastric emptying
C. Gastric pH
D. Drug pH
B. Gastric emptying
Two related drug preparations show comparable ability to reach the systemic circulation in the same amounts and possess similar times to achieve peak plasma concentration. Such drugs are considered as being
A. very hydrophilic
B. bioavailable
C. bioequivalent
D. therapeutically equivalent
C. bioequivalent
Treatment of acute methamphetamine toxicity can be done by
A. neutralization of urine
B. acidification of urine
C. alkalization of urine
D. increased bile secretion
B. acidification of urine
Which of the following organs would distribution of a drug be greatest in terms of blood flow: mass ratio?
A. Brain
B. Kidney
C. Liver
D. Heart
B. Kidney
There are a lot of drugs that manifest delayed toxicity because of altered ADME and half-life. Which of the following drugs has the highest half-life?
A. Aspirin
B. Valproic acid
C. Levothyroxine
D. Paracetamol
C. Levothyroxine
Elevated levels of lead in the blood may cause vomiting, muscle weakness, seizures, and coma. It is best classified as a/an:
A. toxin
B. inorganic poison
C. nutraceutical
D. xenobiotic
B. inorganic poison
A 55-year-old patient was taking aspirin for secondary prevention of stroke. He went to the dentist for tooth extraction but was asked to obtain medical clearance from an internist. He was told to discontinue aspirin for the next 7-10 days before the operation because the medical doctor is sufficiently knowledgeable about the presence of which type of bonds between aspirin and cyclooxygenase in platelets?
A. Covalent bonds
B. Hydrophobic bonds
C. Hydrogen bonds
D. Ionic bonds
A. Covalent bonds
Which of the following types of drugs will have maximum oral bioavailability?
A. Highly hydrophilic bonds
B. Chemically unstable drugs
C. Drugs with high first-pass metabolism
D. Largely hydrophobic, yet soluble in aqueous solutions
D. Largely hydrophobic, yet soluble in aqueous solutions
A patient with epilepsy was maintained on phenytoin and has been seizure-free for a couple of years already. He was diagnosed with PTB and was treated with category I regimen which includes rifampin among others. 2 weeks into the regimen, the patient had sudden recurrence of seizures. What is the best explanation for his condition?
A. Rifampin and phenytoin are inducers of CYP3A4
B. Rifampin and phenytoin are metabolized by the same enzyme
C. Rifampin is a competitive inhibitor of the phenytoin receptor
D. Rifampin is an inducer of CYP2C9
D. Rifampin is an inducer of CYP2C9
Which of the following drugs has the highest volume of distribution?
A. Heparin
B. Alteplase
C. Gentamycin
D. Ethanol
D. Ethanol
A new statin, one of the drugs used in the treatment of myocardial infarction, is being studied by a pharmaceutical company. If a clinical trial would be developed, which of the following would be used as a surrogate endpoint?
A. Lowering of LDL cholesterol levels of subjects
B. Reduction in the incidence of myocardial infarction
C. Decrease in the mortality rate of the subjects enrolled in the study
D. Increase in gap-years in the development of cardiac symptoms
A. Lowering of LDL cholesterol levels of subjects
A downward shift of the Emax accompanied with no shift of EC50 values (unless spare receptors are present) are characteristics of
A. irreversible antagonist
B. allosteric antagonist
C. competitive antagonist
D. physiologic antagonist
A. irreversible antagonist
B. allosteric antagonist
Which of the following statements is correct with regards penicillin?
A. Its use should always be complemented by monitoring an appropriate clinical marker
B. It has a large clinical therapeutic index
C. Its log concentration in plasma to obtain maximal efficacy overlaps with the undesirable effects
D. It has a very narrow population therapeutic window
B. It has a large clinical therapeutic index
Which of the following statements is true with regards a partial agonist?
A. Has always lesser affinity than the full agonist
B. Obtains the same degree of saturation with a full agonist
C. Selectively binds to the inactive form of the receptor
D. May act as an antagonist of the full agonist
D. May act as an antagonist of the full agonist
Using the figure below, drug A mimics the physiologic ligand. Which of the following statements is true?
A. Drug B is a full agonist
B. Drug C is an allosteric antagonist
C. Drug C is an inverse agonist
D. Drug B is a partial agonist
A. Drug B is a full agonist
Which carrier is used by metformin for transport?
A. SLC8
B. SLC28A1
C. MDR1
D. SLC22A1
D. SLC22A1
Which of the following types of drugs will have maximum oral bioavailability?
A. Largely hydrophobic, yet soluble in aqueous solutions
B. Highly hydrophilic drugs
C. Chemically unstable drugs
D. Drugs with high first-pass metabolism
A. Largely hydrophobic, yet soluble in aqueous solutions
Which serves as the major carrier for acidic drugs?
A. Globulins
B. Lipoproteins
C. Alpha 1 acid glycoprotein
D. Albumin
D. Albumin
Which serves as the major carrier for basic drugs?
A. Globulins
B. Lipoproteins
C. Alpha 1 acid glycoprotein
D. Albumin
C. Alpha 1 acid glycoprotein
A 55-year old patient was taking aspirin for secondary prevention of stroke. He went to the dentist for tooth extraction but was asked to obtain medical clearance from an Internist. He was told to discontinue aspirin for the next 7-10 days before the operation because the medical doctor is sufficiently knowledgeable about the presence of which type of bonds between aspirin and cyclooxygenase in platelet?
A. Hydrophobic bonds
B. Covalent bonds
C. Ionic bonds
D. Hydrogen bonds
B. Covalent bonds
A new statin, one of the drugs used in the treatment of myocardial infarction, is being studied by a pharmaceutical company. If a clinical trial would be developed, which of the following would be used as a surrogate endpoint?
A. Reduction in the incidence of myocardial infarction
B. Decrease in the mortality rate of the subjects enrolled in the study
C. Increase in gap-years in the development of cardiac symptoms
D. Lowering of LDL cholesterol levels of subjects
D. Lowering of LDL cholesterol levels of subjects
Alkalization of urine by giving bicarbonate is used to treat patients presenting with acetylsalicylic acid (aspirin) overdose. Which of the following best describes the rationale for alkalization of urine in this setting?
A. To decrease proximal tubular secretion
B. To increase ionization
C. To increase glomerular filtration
D. To increase tubular reabsorption
B. To increase ionization
Elevated levels of lead in the blood may cause vomiting, muscle weakness, seizures, and coma. It is best classified as a/an:
A. Toxin
B. Nutraceutical
C. Inorganic poison
D. Xenobiotic
C. Inorganic poison
Most drugs have molecular weights between 100 – 1000. This upper limit prevents the drug from:
- Moving from one body compartment to another
- Dissociating until it reaches the target organ
- Being prematurely cleared from the circulation
- Binding to other receptors
- Moving from one body compartment to another
- Dissociating until it reaches the target organ
- Being prematurely cleared from the circulation
Naproxen sodium and Mefenamic acid are nonsteroidal anti-inflammatory drugs (NSAIDs). If 550mg of Naproxen causes the same analgesic response as 500mg of Mefenamic acid, which of the following statements is correct about Mefenamic acid?
A. It is more potent and efficacious than Naproxen
B. It is more efficacious than Naproxen
C. It is more potent than Naproxen
D. It is a full agonist while Naproxen is a partial agonist
C. It is more potent than Naproxen
The kidney is the major route of elimination for at least ___ of drugs administered to humans:
A. 1/2
B. 1/4
C. 2/3
D. 1/3
B. 1/4
This branch of pharmacology deals with the undesirable effects of chemicals on an organism:
A. Pharmacogenomics
B. Medical Pharmacology
C. Toxicology
D. Pharmacoepidemiology
C. Toxicology
Which among the phases of clinical trials usually involves healthy volunteers?
A. IV
B. I
C. II
D. III
B. I
Which of the following is a measure of drug safety?
A. EC50
B. Emax
C. ED50
D. TD50/ED50
D. TD50/ED50
Which of the following ligands activates receptor tyrosine kinases?
A. Leukotriene
B. Dopamine
C. Insulin
D. Acetylcholine
C. Insulin
Which of the following organs would distribution of a drug be greatest in terms of blood flow: mass ratio?
A. Kidney
B. Brain
C. Liver
D. Heart
A. Kidney
Which of the following statements is correctly associated with phase II and III clinical trials?
A. May involve hundreds of healthy subjects
B. Randomized, controlled and blinded
C. Detects new indications, risks and optimum doses
D. Determines efficacy and mechanism of action in
animals
B. Randomized, controlled and blinded
Practical knowledge about enantiomers among drugs is important because there is stereoselectivity among:
- Drug-metabolizing enzymes
- Drug transporters
- Drug receptors
- Drug tests
- Drug-metabolizing enzymes
- Drug transporters
- Drug receptors
Which of the following statements is correct about the enantiomers of Carvedilol?
A. The enantiomers are equally potent as beta blockers
B. The S(+) enantiomer is more potent as an alpha blocker than as a beta blocker
C. The R(+) enantiomer is 100-fold more potent as a beta blocker
D. The enantiomers are relatively equipotent as alpha blockers
D. The enantiomers are relatively equipotent as alpha blockers
The most common mechanism for drug absorption from the GI tract is dependent on:
- Membrane surface area
- Concentration gradient
- Solubility coefficient
- Carriers
- Membrane surface area
- Concentration gradient
- Solubility coefficient
Which of the following routes of drug administration reduces hepatic first-pass loss by more than 50%?
- Inhalational
- Oral
- Sublingual
- Rectal
- Inhalational
3. Sublingual
Which of the following parameters determines graded dose-response relationships?
A. Therapeutic index
B. Efficacy
C. Bioequivalence
D. Clearance
B. Efficacy
A downward shift of the Emax accompanied with no shift of EC50 values (unless spare receptors are present) are characteristics of:
A. Inverse agonists
B. Competitive antagonists
C. Allosteric antagonists
D. Physiologic antagonists
C. Allosteric antagonists
Drug X is said to achieve maximal efficacy when:
- All physiologic receptors for drug X are fully saturated
- Affinity exceeds saturation for drug X
- No increase in response happens when a higher concentration of drug X is obtained
- Repeated administration of drug X results to downregulation of receptors
- All physiologic receptors for drug X are fully saturated
3. No increase in response happens when a higher concentration of drug X is obtained
The process of using chemicals for therapeutic effect on a patient is a scope of
A. Medical pharmacology
B. Pharmacogenetics
C. Pharmacoepidimiology
D. Toxicology
A. Medical pharmacology
Which of the ff depicts the effects of a drug depending on its concentration?
A. Graded Dose-Response Curve - Depiction of the observed effects of a drug as a function of its concentration in the receptor compartment
B. Quantal Dose-Response Curve All or none curve: relationship between dose and biologic unit
C. Therapeutic Window Concentration range of a drug that provides efficacy without unacceptable toxicity
D. Therapeutic Index Depicts how selective a drug is in producing its desired effect vs its adverse effects
A. Graded Dose-Response Curve - Depiction of the observed effects of a drug as a function of its concentration in the receptor compartment
A 55 year old patient was taking aspirin for secondary prevention of stoke. He went to the dentist for tooth extraction but was asked to obtain medical clearance from an internist. He was told to discontinue aspirin for the next 7-10 days because the medical doctor is sufficiently knowledgeable about aspirin in terms of
A. Drug size
B. Drug shape
C. Drug transporter
D. Drug-receptor bond
D. Drug-receptor bond
Which of the following transporters is used by digoxin in secondary active transport?
A. MDR1
B. SLC8
C. SLC22A1
D. SLC28A1
B. SLC8
Adrenocorticotropic hormones stimulate the release of glucocorticoids by acting on the:
A. Zona Glomerularis
B. Zona Fasiculata
C. Adrenal Capsule
D. Adrenal Medulla
B. Zona Fasiculata
Chlorothiazide is a weakly acid drug. If administered orally, which route of absorption would directly pass it to the parenchyma?
A. Mouth
B. Stomach
C. Duodenum
D. Jejunum
B. Stomach
The kidney is the major route of elimination of ____of drugs administered.
A. 20-25%
B. 25-30%
C. 30-35%
D. 35-40%
A. 20-25%
Ibuprofen and mefenamic acid are non steroidal anti inflammatory drugs (NSAIDs). If 400mg of ibuprofen can produce the same analgesic response as 500mg of mefenamic acid, which of the following statements is correct?
A. Ibuprofen is more potent than mefenamic acid
B. Ibuprofen is more efficaceous than mefenamic acud
C. Ibuprofen if a full agonist while mefenamic acud is a partial agonist
D. Ibuprofen is a better drug to take for pain relief than mefenamic acid
A. Ibuprofen is more potent than mefenamic acid
Which of the following principles should be present in the conduct of clinical trials?
- Avoidance of placebo controls
- Return of investment
- Use of surrogate end points
- Informed consent
- Avoidance of placebo controls
3. Use of surrogate end points
True of graded dose - response relationship
- Efficacy
- Clearance
- Potency
- Therapeutic Index
- Efficacy
3. Potency
Quantity of drug reaching systemic circulation/ Quantity of drug administered
A. Absorption
B. Distribution
C. Metabolism
D. Excretion
A. Absorption
Defined as the fluid volume that is required to contain the entire drug in the body at the same concentration measured in the plasma
A Absorption B Distribution C Metabolism D Excretion E None of these
B Distribution
Atropine
A. GPCR B. Ion Channel C. Nuclear Receptor D. Receptor tyrosine kinase Pharmacology
A. GPCR
L-thyroxine
A. GPCR
B. Ion channel
C. Nuclear receptor
D. Receptor tyrosine kinase
C. Nuclear receptor
Lidocaine
A. GPCR
B. Ion channel
C. Nuclear receptor
D. Receptor tyrosine kinase
B. Ion channel
Nicotine
A. GPCR
B. Ion channel
C. Nuclear receptor
D. Receptor tyrosine kinase
B. Ion channel
Activity of the drugs in relation to adrenergic receptors:
Terazosin and Norepinephrine
A. Full agonist
B. Partial agonist
C. Competitive antagonist
D. Non-competitive antagonist
C. Competitive antagonist
Activity of the drugs in relation to adrenergic receptors:
Histamine and Epinephrine
A. Full agonist B. Partial agonist C. Competitive antagonist D. Non-competitive antagonist E. Functional antagonism
E. Functional antagonism
Activity of the drugs in relation to adrenergic receptors:
Phenylephrine and norepinephrine
A. Full agonist B. Partial agonist C. Competitive antagonist D. Non-competitive antagonist E. Functional antagonism
A. Full agonist
