ESA 4 - CPT Flashcards
1) A 46 year old is currently taken atorvastatin to reduce his cardiovascular disease risk. He has been experiencing low mood and purchased St John’s Wort which he has been taking for 7 days. It is known that St John’s Wort is an inducer of CYP3A4.
t1/2 = 0.7x Vd/CL.
In this patient, what best describes the effect of the St John’s Wort on the individual terms in the equation for half-life for the statin.
A. Nothing changes all the terms remain the same
B. t1/2 decreases, all other terms remain the same
C. t1/2 decreases, Vd increases CL remains the same
D. t1/2 remains the same, CL increases Vd increases
E. t1/2 decreases, CL increases Vd remains the same
Answer is E. Half-life will decrease as metabolism is increased and therefore excretion. Clearance will go up (inversely proportional to (t1/2) Vd unchanged.
2) A diabetic patient is started on treatment with a sulfonylurea. Which of the following statements is correct about the pharmacological action in pancreatic ß-cell by sulfonylureas?
A. ATP sensitive K+ channel activity is agonised increasing insulin release into circulation
B. ATP sensitive K+ channel activity is antagonised, decreasing K+ efflux and increasing insulin release
C. ATP sensitive K+ channel activity is agonised to decrease K+ efflux which increases insulin release
D. Depolarisation decreases both Ca2+ entry and insulin vesicle fusion rate with the cell membrane
E. Depolarisation increases both Ca2+ entry and K+ efflux, which increase insulin release into the circulation
Answer is B.
3) A 58 year old male with type 2 diabetes has a total cholesterol of 6.8 mmol/L. He does not have established cardiovascular disease but his CVD risk score is 14%. What cholesterol lowering therapeutic would you try first?
A. Atorvastatin B. Fenofibrate C. Ezetimibe D. Cholestyramine E. Simvastatin
Answer is A. Statin is most effective option for lowering LDL cholesterol. Fenofibrate would be more appropriate for triglyceride reduction. Cholestyramine (bile acid binding resin) will reduce LDL cholesterol but only by ~ 20% and is not recommended as a first line primary prevention. Simvastatin would reduce LDL cholesterol by the same HMGCoA reductase inhibition as atorvastatin but is less potent (~30 vs 40% reduction in LDL-C at 20 mg dose) which is recommended for type 2 diabetics with no established CVD but a CVD risk score of >10%.
4) A 69 year female with atrial fibrillation reports no episodes of palpitations and does not have any other cardiovascular disease. Which antiarrhythmic agent would you prescribe to control rate for this patient?
A. Flecainide B. Bisoprolol C. Amiodarone D. Digoxin E. Ivabradine
Answer is B. Bisoprolol beta blocker for rate control. Flecainide would be appropriate for rhythm control as would amiodarone. Digoxin is not a first line primary rate control agent. Ivabradine (if current inhibition) used for sinus tachycardia and rate reduction in HF or ACS.
5) A 60 year old male has stage b heart failure (structural disease with no symptoms). In addition to an ACE inhibitor, his cardiologist suggests that he take a bet blocker as well. Which of the following is not true of the therapeutic benefit of beta blockers in the management of heart failure?
A. Decrease heart rate B. Inhibit the effects of noradrenaline on cardiac muscle remodelling C. Increase renin release D. Improve systolic function E. Decrease afterload
Answer is C. beta blockers will decrease renin release which decrease sympathetic output, decrease sodium and water retention, increase bradykinin and vasodilation. All others are true
6) Which diuretic is used as an add-on therapy in resistant hypertension (blood pressure not adequately reduced with three first line drugs)?
A. Indapamide B. Furosemide C. Bendroflumethiazide D. Spironolactone E. Amiloride
Answer is D. spironolactone. Evidence suggests that this potassium sparing diuretic can be effective as an add-on once an A C and thiazide like D have been exhausted.
7) Naloxone has been prescribed for a patient admitted to A&E who is suspected of taking an overdose of morphine. It is hoped that the naloxone will reverse the respiratory depression that the patient is presenting with. Dose escalation may be needed if there is little response. Which of the below best describes naloxone in this situation?
Naloxone is a non-competitive antagonist Naloxone is a more potent agonist Naloxone shows greater efficacy than morphine Naloxone has less affinity than morphine Naloxone is a competitive antagonist
Answer is E. Naloxone is a competitive antagonist, non-selective for all opioid receptors.
8) A 44 year old male has been for a health MOT and has been diagnosed with essential hypertension. His blood pressure has been confirmed following ABPM as 158/95. The GP prescribes losartan. Which of the below best describes how it is hoped losartan will reduce his blood pressure?
A. Losartan will inhibit angiotensin converting enzyme
B. Losartan will inhibit calcium channels in vascular smooth muscle cells
C. Losartan will potentiate the action of aldosterone
D. Losartan will inhibit the AT1 receptor
E. Losartan will inhibit the adrenergic stimulation of vascular smooth muscle
The answer is D. Losartan is an angiotensin II receptor antagonist (AT1 receptor), preventing action of ATII. All others are mechanisms of action of other antihypertensive class apart form C which would exacerbate the hypertensive state
9) A 54 year old female is visiting her GP practise to have her blood pressure medication reviewed. She currently takes the lowest recommended dose of amlodipine hydrochloride and confirms that she is adherent. Her blood pressure is confirmed to be 145/92. A small reduction on the measurement recorded at her last appointment 3 months ago. What should be recommended?
A. Increase the dose of amlodipine hydrochloride
B. Continue taking the same dose of amlodipine hydrochloride and review in 3 months.
C. Add an ACE inhibitor or ARB
D. Add a thiazide like diuretic
E. Swap the amlodipine hydrochloride for an ACE inhibitor or ARB
The answer is A. The next step should be to increase the dose of the CCB, ensure adherence before adding a second agent.
10) A 36 year female has been admitted to a general ward with a severe infection. She has been prescribed i.v. antibiotics. A steady state plasma concentration is reached in 5 hours. What would be the predicted half-life of the antibiotic?
A. 10 hours B. 25 hours C. 1 hour D. 15 hours E. 7.5 hours
The answer is C. 1 hour. CpSS should be reached in approximately 5 half-lives. 5/5=1.
11) A junior doctor is reviewing the medications of an elderly patient. The patient reports that they have stopped taken one of their medications because it was causing side effects described as shaking or tremor. The doctor ascertains that it is a type B adverse drug reaction and goes about reporting it to the Medical and health Products Licensing Agency through the online yellow card system. Which of the below does NOT describe a type B ADR?
A. Dose-related B. Uncommon C. Unpredictable D. Serious/irreversible E. Associated with high mortality
Answer is A. Type B ADRs are not dose related, they are unpredictable and idiosyncratic.
12) A clinical pharmacologist has been in discussion with a 59 year male about the management of his cholesterol levels as part of secondary prevention following an AMI 9 months ago. He already takes statin, but has struggled to tolerate a dose that is needed to reduce cholesterol sufficiently. The pharmacologist suggests adding ezetimibe to a lower dose of atorvastatin. There is evidence that this combination produces synergistic effects. How does the ezetimibe work in this patient?
A. Inhibits the rate limiting step in the mevalonate pathway
B. Activate the gene transcription factor PPARα
C. Inhibits hepatic diacylglycerol acetyltransferase-2
D. Inhibiting the PCSK9 protein
E. Inhibiting NPC1L1 transporter
The answer is E. Acts at the brush border of the small intestinal mucosa inhibiting NPC1L1 transporter which is proposed to be the limiting protein in GI cholesterol absorption. All others are mechanisms of other hyperlipidaemia therapeutics.
13) Which of the following is not an ADR of hormone replacement therapies prescribed during menopause.
A. Increased risk of ischaemic heart disease B. Increased risk of breast cancer C. Increased risk of venous embolism D. Increased HDL-C E. Increased risk of ovarian cancer
The answer is D. in some preparations the effects are less marked but overall there is an increase in HDL-C which is may improve cardiovascular disease risk. Is not an adverse drug reaction.
14) Which clotting factor does low molecular weight heparin (LMWH) target specifically and the reason why it requires much less monitoring than UFH?
A. Xa B. IIa C. XIa D. XIIa E. IXa
The answer is A. LMWH selectively accelerates interaction between antithrombin and factor Xa.
15) A study was carried out to compare the vital capacity of coal miners to the vital capacity of farm workers aged 30-39. The study measured the vital capacity of 100 workers from each occupation. Other factors that might affect vital capacity are smoking, exercise and age. The smoking habits of the two worker types are similar, but the coal miners generally exercise less than the farm workers.
Which of the following is a confounding variable in this study?
A. Exercise B. Vital capacity C. Smoking habit. D. Occupation E. Age
The answer is A. Exercise status may contribute to differences in vital capacity. The exercise status of the two groups is likely to be different. Vital capacity is the variable being measures. Age and smoking have been accounted for (loosely for smoking) and occupation is the comparator.
- If 2.5 mg ramapril produces the same blood pressure lowering affect as 10mg lisinopril, which is correct?
A. Ramapril is more potent than lisinopril
B. Ramapril is more efficasios than lisinopril
C. Ramapril is a full agonist and lisinopril is a partial agonist
A. A drug that causes the same affect at lower doses is more potent. Maximal drug effects would be needed to conclude if b or c were correct.
- A new antibiotic produces toxic affects at a dose of 120 mg TDS in 50% of patients and a clinically desired response at 100 mg TDS in half of the populaton. What is the therapeutic index of this new antibiotic?
A. 1.2
B. 0.83
C. 1.0
A. Therapeutic index is equal to dose that produces toxicity in 50% population/dose that produces clinically desired effect.
- Buprenorphine is a partial agonist for opioid receptors. Can it have an affinity for these receptors that is greater than a full agonist such as codeine?
A. True
B. False
A. Partial agonists can have greater, the same or lower affinity for the same receptor as a full agonist but will have lower efficacy than the full agonist.
- Plasma steady state is reached quicker if the rate of infusion of an i.v. drug is doubled.
A. True
B. False
B. The plasma steady state will increase (will be doubled), but will take just as long to be reached as if the rate was halved.
- The P450 enzyme CYP3A4 is inhibited by grapefruit juice. How would this affect the plasma concentration of simvastatin if a patient were to drink grapefruit juice alongside taking this daily statin?
A. CYP3A4 is not involved in statin metabolism so will not have an affect
B. It could increase plasma concentrations of simavastatin
C. It could decrease plasma concentrations of simvastatin
B. Simvastatin metabolism is in part due to CYP3A4. Inhibition with grapefruit juice could result in elevated plasma concentrations of this statin.
- Steady state plasma concentration will be reached in how many half lifes?
A. 1
B. 3
C. 5
C. Ultimate steady state 100%: 1 t1/2 (100/2) = 50% 2 t1/2 (50 + 50/2) = 75% 3 t1/2 (75 + 25/2) = 87.5% 4 t1/2 (87.5 + 12.5/2) = 93.8% 5 t1/2 (93.75 +6.25/2) = 96.9%
- Liphophilic drugs will readily cross through cell membranes.
A. True
B. False
A. Lipophilic drugs dissolve in the lipid membrane and penetrate the cell surface.
- A patient is taking 80mg atorvastatin for secondary cardiovascular disease prevention. Only 11.2 mg is absorbed unchanged due to incomplete gut absorption and gut wall excretion. What is the oral bioavailability of atorvastain?
A. 100%
B. 7%
C. 14%
C. Bioavailability is the rate and extent at which drug reaches the systemic circulation. Total drug given orally/drug given i.v.(100% bioavailability)X100 = 11.2/80X100=14%
- A 46 year old female patient (70 kg) is prescribed ramapril to manage essential hypertension. Her dose has been increased to 5mg OD. The peak plasma concentration of ramapril was 0.06 mg/L. The apparent volume of distribution is:
A. 1.2 L/kg
B. 84 L/kg
C. 17 L/kg
A. Vd= dose/plasma concentration = 5/0.06 = 83.3 L. Patient is 70 kg, so 84/70 is ~ 1.2 L/kg
- Which of the following reactions is likely to occur during Phase II drug metabolism
A. Oxidation
B. Reduction
C. Glucuronidation
C. Phase II metabolism involves conjugation reactions. Sulfation and gulcuronidation are the most common. Oxidation or reduction occur during Phase I metabolism.
- Which of the following is not a known reaction between beta blockers and thiazide diuretics?
A. Hyperglycaemia
B. Hyperlipideamia
C. Hyperkalaemia
C. Thiazides are likely to cause hypokalaemia and beta blockers don’t directly affect this action.
- Which of the below is a common ADR of furosemide?
A. Increased LDL cholesterol
B. Hypercalaemia
C. Impotence
A. B and C are common ADRs associated with Spironolactone
- Labetalol can be used to treat hypertension during pregnancy
A. True
B. False
A. Oral lebetalol can be used to treat gestational hypertension when other agents (ACEi and ARBs, CCBs) are contraindicated.
- NICE guidelines define hypertensiton as
A. >130/90
B. >140/90
C. >120/80
B. 120/80 deemed “normal” ideal for reducing risk of CVD. 130/90 is designated prehypertension, which should be targeted with lifestyle interventions.
- Resistance to blood flow is affected most by
A. Length of the vessel
B. Class of vessel (named artery, arteiole, capilary etc.)
C. Radius of the vessel
C. Part of Poiseuille’s law demonstrates that resistance to flow is inversely proportional to the radius of the vessel to the fourth power. Small changes in radius result in big differences in resistance to flow.
- Beta blockers are used in treating left ventricular heart failure by increasing heart rate?
A. True
B. False
B. Slightly counterintuitively, beta blockers slow the heart, allowing more time for filling and increasing cardiac output.
- Spironolactone affords its initial blood pressure lowering action by:
A. causing hyperkalaemia
B. blocking clacium entry into vascular smooth muscle cells
C. Inhibition of aldosterone activity
C. Although not first line therapy, spironolactone inhibits aldosterone activity at its receptor leading to diuresis. Long term it is suggested that it may have direct effects on the vasculature.
- ACE inhibitors can lower blood pressure by inhibiting the brakdown of bradykinin?
A. True
B. False
A. ACE inhibitors can lower blood pressure by inhibiting the breakdown of bradykinin as well as their action through ACE inhibition.
- Which class of drugs does losartan belong too?
A. ACE inhibitors
B. angiotensin receptor blockers
C. aldosterone receptor antagonists
B.
- Which of the following calcium channel blockers (CCBs) shows greatest selectivity for vascular smooth muscle?
A. amlodopine
B. verapamil
C. diltiazem
A. Amlodopine is a dihydropyridine like calcium channel blocker that shows little to no acttivity in the cardiac tissues. Verapamil shows selectivity for cardiac tissue with some VSM action and diltiazem sits between them.
- Oestrodiol’s major effects do not include:
A. Stimulation of growth of the endometrium
B. Stimulates production of progesterone receptor
C. Inhbition of esrogen receptor production
C. Progesterone acts to inhibit production of the estrogen receptor.
- Testosterone
A. Increases HDL:LDL ratio
B. Decreases HDL:LDL ratio
C. Has no affect on cholesterol profile
A. Increased ratio ( less HDL to other cholesterol) increasing risk of atherosclerotic disease i
males.
- Combined oral and progesterone only contraceptive efficacy is _________ by antiepileptic drugs including phenytoin
A. Increased
B. Decreased
C. No change
B. Phenytoin among other drugs increase CYP450 activity which increases metabolism of COCP and POP resulting in reduced efficacy
- Hormone replacment therapy can decrease the risk of venous thromboembolism?
A. True
B. False
B. Increased risk though effects on a number of proteins in the clotting cascade including increased thrombin activity.
- A type A adverse drug reaction is not
A. Rare
B. Predictable
C. Dose dependent
A. Type A ADRs are predictable and dose dependent. With our clinical knowledge we should be able to foresee them happening, Especially with a clinical history and knowledge of other agents being taken.
- The yellow card system is the responsibility of healthcare professionals only.
A. True
B. False
B. Although the majority of reports are likely to come through health care professionals, patients and carers can and should report ADRs through this scheme too.
- Tamoxifen is
A. Is a pure agonist of the oestrogen receptors
B. Is a pure oestrogen receptor antagonist
C. Is a selective oestrogen receptor modulator
C. Depending on the tissue, tamoxifen acts as an antagonist (breast tissue) or an agonist (endometrium)
- Oestrogens and their synthetic analogues are not well absorbed in the GI tract.
A. True
B. False
B. They are well absorbed in the GI tract and undergo significant first pass metabolism in the liver.
- Like >10% of Africans, a man from Ethiopa has the common deffieiceny in CYP2D6. What effect if any would you expect to see if he was using codeine as an analgesic?
A. Increased therapeutic benefit, a lower dose may be considered
B. Decreased therapeutic effect, an increased dose may be considered
C. the analgeisc properties of codeine are not affected by CYPD6 deficiency
B. The active metabolite of codeine requires CYP2D6 oxidation activity. A deficiency would result in less active metabolite being produced and less analgesia.
- In a patient with hepatic disease, what effect will this have on the therapeutic action of tamoxifen?
A. Increased
B. Deacreased
B. tamoxifen is a pro drug that relies on hepatic metabolism to produce active metabolites.
- GLP-1 agonists like exenatide have shown promising weight reduction effects during long term use. Their actions include
A. Decreased insulin secretion
B. Decreased gastric emptying
C. Increased glucagon production
B. GLP-1 agonists increase insulin secretion and decrease glucagon secretion. Decreased gastric emptying decreases postprandial glycaemia.
- Glucagon raises blood glucose levels in patients who have severe insulin induced hypoglycaemia.
A. True
B. False
A. Glucagon can be administered i.m., s.c. or i.v. Glycogon synthesis is reduced blocking the effects of insulin in the liver.
- Glicazide is a sulfonylurea. Which of the following is not a primary concern when prescribing it for diabetic managment?
A. Cause hypoglycaemia
B. Contraindicated in renal impariment
C. Cause weight gain
B. Gliclazide is metabolised hepatically so can be used in renally compromised patients with care. Sulfonylureas cause weight gain and relativley more likely to cause hypoglycaemia than metformin.
