Final Exam: Atkins Flashcards
Compare dobutamine and dopamine:
1) Which is the pure beta-2 antagonist?
2) Which has significant metabolism by enzymes in neural tissue?
3) Which is the commercially available prep. available as a mixture of stereoisomers
1) Which is the pure beta-2 antagonist? NONE
2) Which has significant metabolism by enzymes in neural tissue?
B
3) Which is the commercially available prep. available as a mixture of stereoisomers
A
Where do inhibitors of ENac act?
Collecting duct
Where do early carbonic anhydrase inhibitors (which cause systemic acidosis) act?
Proximal convoluted tubule
Where do high ceiling diuretics act?
Ascending limb of Henle
Where do early carbonic anhydrase inhibitors (now used for glaucoma) act?
Proximal convoluted tubule
Where to aldosterone antagonists act?
Collecting duct
Where to thiazides and hydrothiazides act?
Distal convoluted tubule
Answer true or false about enalapril:
1) Has the advantage of not causing a dry cough as a side effect.
2) Has a short half-life due to its tendency to form disulfides
3) Was the first “carboxyl” ACE inhibitor
1) Has the advantage of not causing a dry cough as a side effect
FALSE
2) Has a short half-life due to its tendency to form disulfides
FALSE
3) Was the first “carboxyl” ACE inhibitor
TRUE
What is the active form of enalapril? What is the function of the active drug?
Ethyl ester is converted to carboxylic acid.
It chelates Zn2+ in the active side of ACE
All injectable anesthetics: A) have protonatable amines B) have xylylamides C) inhibit T-type Ca2+ channels D) all of the above
A) have protonatable amines
The anticoagulant activity of heparin results from its ability to ________ antithrombin III. (Activate/Inhibit)
Activate
The _______ charge of protamine results in it having a high affinity for heparin, which makes it a good antidote for heparin-induced hemorrhage. (Positive/Negative)
Positive
The pentasaccharide that is critical for heparain activity includes ________ charged functional groups in a specific spatial orientation that is difficult to recreate synthetically. (Negatively/Positively)
Negatively
Answer each statement with urokinase, streptokinase, recombinant tPA, multiple or none.
A) The most fibrin-specific
B) Can be pyrogenic or antigenic
C) A human enyzme that directly cleaves plasminogen w/o binding to fibrin
D) Cleaves plasminogen activator inhibitor-1
E) Has a short half-life requiring IV drip to maintain thrombolytic effects
A) The most fibrin-specific: TPA
B) Can be pyrogenic or antigenic: STREPTOKINASE
C) A human enyzme that directly cleaves plasminogen w/o binding to fibrin: UROKINASE
D) Cleaves plasminogen activator inhibitor-1: NONE
E) Has a short half-life requiring IV drip to maintain thrombolytic effects: UROKINASE, STREPTOKINASE, TPA
Recombinant nonglycosylated human protein produced in bacterial cells. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Reteplase
Full length recombinant human tissue plasminogen activator produced in cultured mammalian cells. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Alteplase
Recombinant tPA without Kringle I and a Finger domain. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Reteplase
An enzyme with a half-life that in some cases allows treatment with a single IV injection followed by transport to a hospital. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Tenekteplase
An enzyme with good fibrin specificity but a short half-life that requires an IV drip enroute to a hospital. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Alteplase
Efficiently penetrates a clot because it has a lower affinity for fibrin. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Reteplase
Recombinant human protein, engineered to have high fibrin specificity, and is not susceptible to inhibition by PAI-1. A) Tenekteplase B) Reteplase C) Streptokinase D) Alteplase Can be none.
Tenekteplase
True or false: Heparin contains a pentasaccharide that is not found in low MW heparins, like enoxaparin.
False
True or false: The negative charges on heparin cause it to bind and inhibit antithrombin III.
False
True or false: Heparin is inhibited by the protein protamine.
True
True or false: Unfractionated heparin is not useful orally because it is poorly absorbed and rapidly degraded at low pH.
True
True or false: Low molecular weight heparin is a recombinant protein that has been engineered for higher affinity for antithrombin III.
False
Directly results in decreased expression of ENaC, without metabolic activation. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
None
A prodrug that is converted to an inhibitor of the aldosterone receptor. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
Spironolactone
Inhibits Na+/Cl- transport in the distal convoluted tubule. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
HCTZ
A substrate for the OCT system. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
Amiloride
A 2-amino-5-sulfamolyl-benzoic acid loop diuretic. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
Furosemide
Metabolized via glucuronidation. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
Furosemide
Inhibits carbonic anhydrase in the proximal convoluted tubule. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
None
Directly inhibits ENaC. A) Furosemide B) HCTZ C) Amiloride D) Spironolactone Can be none
Amiloride
Which are substrates for the OAT system? A) Furosemide B) HCTZ C) Amiloride D) Spironolactone
Furosemide
HCTZ
Which can cause hypokalemia? A) Furosemide B) HCTZ C) Amiloride D) Spironolactone
Furosemide
HCTZ
A prodrug that inhibits neprilysin after activation. A) Enalaprilate B) Captopril C) Fosinopril D) Perindopril Can be one, all or none.
None
Disulfide formation can limit duration of action. A) Enalaprilate B) Captopril C) Fosinopril D) Perindopril Can be one, all or none.
Captopril
An acyl proline that mimics the histidine in the active site of ACE. A) Enalaprilate B) Captopril C) Fosinopril D) Perindopril Can be one, all or none.
None
Causes a dry cough as a side effect. A) Enalaprilate B) Captopril C) Fosinopril D) Perindopril Can be one, all or none.
All
A prodrug that contains a zinc-chelating phosphinate after activation. A) Enalaprilate B) Captopril C) Fosinopril D) Perindopril Can be one, all or none.
Fosinopril
Metabolized via glucuronidation. A) Enalaprilate B) Captopril C) Fosinopril D) Perindopril Can be one, all or none.
All
True or False: Optimal sunscreens induce the synthesis of melanin.
False
True or False: Optimal sunscreens absorb both UVA and UVB light and dissipate the energy as heat.
True
True or False: In PUVA therapy methoxy psoralen forms DNA adducts in skin cells upon exposure to light.
True
True or False: Furanocoumarins are used in photodynamic therapy.
False
True or False: PABA ester sunscreens absorb light of longer wavelength than benzene.
True
True or False: The sunscreen oxybenzone breaks down in UV light, but can be stabilized by the addition of abobenzone.
False
A prodrug requiring activation by CYP2C9. A) Eprosartan B) Valsartan C) Losartan Can be one, all or none
None
The tetrazole is useful for forming salts and for increased bioavailability. A) Eprosartan B) Valsartan C) Losartan Can be one, all or none
B or C
The imidazole mimics histadine in angiotensin II. A) Eprosartan B) Valsartan C) Losartan Can be one, all or none
A or C
An irreversible inhibitor of the organic anion transporter. A) Eprosartan B) Valsartan C) Losartan Can be one, all or none
None
Inhibits angiotensin II subtype 1 receptors. A) Eprosartan B) Valsartan C) Losartan Can be one, all or none
All
Diltiazem is:
A) An aralkylamine L-type Ca2+ channel inhibitor
B) sold as a mixture of 4 stereoisomers with equivalent therapeutic efficacy
C) A bipyridine used for congestive heart failure
D) Metabolized to desacetyl diltiazem, which contributes to the therapeutic activity
E) A beta-2 selective beta blocker
D) Metabolized to desacetyl diltiazem, which contributes to the therapeutic activity
Which of the following is a class 3 antiarrhythmic that causes "smurf syndrome"? A) Procainamide B) Bretylium tosylate C) Amiodarone D) Inamrinone E) Dronedarone
C) Amiodarone
Dihydropyridines (nifedipine):
A) are conformationally rigid and present their target Ca2+ channels with a single conformation to bind
B) undergo CYP-dependent inactivation by oxidation to the corresponding pyridines
C) Inhibit phosphodiesterases
D) Look like cupcakes
E) Are metabolized mainly via glucuronidation at the N-atom of the dihydropyridine ring
B) undergo CYP-dependent inactivation by oxidation to the corresponding pyridines
Organic nitrates, such as isosorbide dinatrate:
A) React with DNA to down-regulate Ca channel expression
B) Inhibit PDE-5 as a result of releasing nitrite ion
C) Are used for CHF
D) React with cellular thios to yield nitrosothiols, which subsequently yield nitric oxide
D) React with cellular thios to yield nitrosothiols, which subsequently yield nitric oxide
Dobutamine is a structural analog of norepinephrine used for acute CHF.
A) Dobutamine and NE undergo similar hepatic CYP-dependent metabolism
B) Dobutamine has positive inotropic effects because it inhibits cardiac Na/K/ATPases
C) Dobutamine is used as a racemic mixture of isomers with a different pharmacology
D) NE and dobutamine are both metabolized primarily by neuronal enzymes such as dopamine beta-hydroxylase and COMT
C) Dobutamine is used as a racemic mixture of isomers with a different pharmacology
Causes a dry cough as a common side effect.
A) ACE
B) ARB
C) Both
A) ACE
Binds to angiotensin II receptors, of subclass (AT-II)I
A) ACE
B) ARB
C) Both
B) ARB
Chelate Zn2+ ions in the active site of its target, in their active form.
A) ACE
B) ARB
C) Both
A) ACE
Analogs of the peptides of angiotensin I or II
A) ACE
B) ARB
C) Both
ARB/Both
An acyl proline that mimics angiotensin I.
A) ACE
B) ARB
C) Both
A) ACE
True or false: only ivabradine inhibits Na+ channels in the SA node (funny channels).
True
True or false: ivabradine is achiral, in contrast to verapamil for which the (S) enantiomer is more potent than the (R) enantiomer.
False (the opposite is true)
True or false: both are alkyl amines that inhibit Ca2+ channels.
False
True or false: Ivabradine is metabolized mainly by N-glucuronidation in contrast to verapamil which is metabolized mainly by CYPS.
False (same metabolism)
True or false: both a metabolized extensively by CYP-dependent N-dealkylation and O-dealkylation.
True
True or false: ivabradine selectively inhibits N-type Ca2+ channels
False (not a ca channel)
Why might you need to use higher doses of local anesthetic in injured tissue than normal tissue? Note that injured tissue has slightly lower pH than normal tissue.
- Have secondary or tertiary amines with pKa 8-9
- At pH 7.4, they are mainly protonated with some neutral species
- The neutral species goes into the membrane and binds to voltage sensitive Na+ channels on inside of neural membrane
- When the pH is lower, there is even less neutral species reducing the concentration of in the cell, so you need higher doses
True or false: synthetic heparins are widely available because it is easy to synthesize the pentasaccharide that is in them.
False
True or false: Low MW heparins have more predictable PK properties.
True
True or false: heparin forms a complex with antithrombin III and makes it a more potent inhibitor of thrombin.
True
True or false: low MW heparins contain the same disaccharide as “normal” heparin.
True
True or false: Antithrombin II is a negatively charged protein and a constituent of normal plasma.
False (positive)
True or false: heparin forms a complex with vitamin K epoxide reductase and makes it a more potent inhibitor of thrombin.
False (complex with antithrombin III)
Often used as a photostabilizer to protect other sunscreen ingredients. A) Melanin B) Padimate C) Oxybenzone D) Avobenzone E) 8-methoxy-psoralen Can be more than one or none
C) Oxybenzone
Absorbs UV light and reacts with O2 or DNA, making it useful in treating psoriasis. A) Melanin B) Padimate C) Oxybenzone D) Avobenzone E) 8-methoxy-psoralen Can be more than one or none
E) 8-methoxy-psoralen
Absorbs UV light and dissipates the energy as heat, without becoming chemically reactive. A) Melanin B) Padimate C) Oxybenzone D) Avobenzone E) 8-methoxy-psoralen Can be more than one or none
A) Melanin
B) Padimate
C) Oxybenzone
D) Avobenzone
Absorbs the widest range of UVA and UVB. A good sunscreen that breaks down in sunlight if not formulated with photostabilizers. A) Melanin B) Padimate C) Oxybenzone D) Avobenzone E) 8-methoxy-psoralen Can be more than one or none
D or D+C
A member of the anthranilate class of sunscreens. A) Melanin B) Padimate C) Oxybenzone D) Avobenzone E) 8-methoxy-psoralen Can be more than one or none
None
What is the importance of the acidic proton in the structure of warfarin?
The anion oxygen left after deprotonation allows warfarin to be formulated as salts in oral tablets. It also results in intramolecular ring closure to generate an additional chiral center. Make clinical use more difficult/complex.
