Drugs for Ischaemic heart disease 2

Question 1

explain what happen with Glyceryl trinitrate

Answer 1

Glyceryl trinitrate – rapidly inactivated by hepatic metabolism

Question 2

The following question are based on Glyceryl trinitrate
RoA for organic nitrates:
Absorbed where:
Ineffective when:
DoA:
Explain the effects of volatility:
Which one is better

Answer 2

• Route of administration: sublingual – onset of action = few minutes
  converted to di- and mononitrates
• Absorbed through the skin – transdermal patch
• Ineffective if administered orally – first pass metabolism by the liver
• Duration of action: 30 minutes
• Due to volatility of the active ingredient, if tablets are opened, the
  volatile substance evaporates
• Spray is better, more stable.

Question 3

organic nitrates that is longer acting, absorbed and metabolised more slowly

Answer 3

Isosorbide mononitrate:

Question 4

RoA for Isosorbide mononitrate

Answer 4

oral

Question 5

When to take Isosorbide mononitrate

Answer 5

take twice daily in the morning (8:00) and at lunch (14:00) to allow
for the nitrate free period (to avoid tolerance)

Question 6

Least lipophilic cardio-selective β1 blocker – loses selectivity at high
doses

Answer 6

Atenolol

Question 7

Pks for Atenolol

Answer 7

• Give once daily
• Excreted mainly unchanged in the urine – may accumulate in kidney
  failure

Question 8

Not affected by liver disease, or drugs inhibiting hepatic metabolism
or conditions affecting hepatic blood flow
Name that drug

Answer 8

Atenolol

Question 9

Contra-indication for atenolol

Answer 9

Contraindicated in heart block, symptomatic heart failure (unless or
until signs are controlled), sinus bradycardia, cardiogenic shock

Question 10

Caution for atenolol

Answer 10

• Cautions: renal failure, pregnancy

Question 11

Drug interatcion for Atenolol

Answer 11

Drug interactions:
* Digoxin, verapamil, diltiazem additive depressant effects on the heart;
* Insulin / oral antidiabetics, increased risk of hyperglycaemia and masking of
hypoglycaemia (except sweating)

Question 12

Adverse effects for Atenolol

Answer 12

Adverse effects: Decreased HDL, increased TGs and glucose utilization
impairment, bronchospasm (asthma, high doses)

Question 13

Explain the ACS

Answer 13

Acute reduction in coronary blood flow most often due to a ruptured
atherosclerotic plaque and subsequent formation of an intracoronary
thrombus. The reduction in coronary blood flow produces myocardial
ischemia and, if left untreated, may lead to myocardial infarction (MI).

Question 14

List the spectrums of ACS
3 marks

Answer 14

• Unstable angina (UA)
• Non-ST-segment elevation myocardial infarction (NSTEMI)
• ST-segment elevation myocardial infarction (STEMI),

Question 15

Explain the unstable angina and also the additional characteristics

Answer 15

Unstable angina is a medical emergency and if untreated can progress
to NSTEMI. Presents as chest pain or discomfort like stable angina but
with the following additional characteristics:
* angina at rest or minimal effort
* angina occurring for the first time, particularly if it occurs at rest
* prolonged angina > 10 minutes, not relieved by sublingual nitrates
* the pattern of angina accelerates and gets worse

Question 16

Explain the short term goal for ACS treatment

Answer 16

Short-term goals:
* Early restoration of blood flow to the infarct-related artery to prevent
infarct expansion (in the case of MI) or prevent complete occlusion and MI
(in UA);
* Prevention of death and other MI complications;
* Prevention of coronary artery re-occlusion
* Relief of ischemic chest discomfort.

Question 17

Explain the long-term goals for ACS treatment

Answer 17

Long-term goals:
* Control of atherosclerosis risk factors,
* Prevention of additional MACE, including reinfarction, stroke, and HF
* Improvement in quality of life.

Question 18

List the MONA(older acronym) for ACS acute supporative care

Answer 18

MONA (older acronym)
* Morphine
* Oxygen
* Nitroglycerin
* Aspirin

Question 19

List the THROMBINS2 (newer acronym)

Answer 19

THROMBINS2 (newer acronym)
* Thienopyridine (clopidogrel)
* Heparin
* RAAS
* Oxygen
* Morphine
* B-blocker
* Intervention
* Nitroglycerin
* Statin/salicylate

Question 20

List the Initial management of unstable ANGINA PECTORIS &
NSTEMI

Lots but say what you can remember

Answer 20

• Oxygen 40% via facemask, if saturation < 94% or if in distress.
• Aspirin, oral, 150 mg as a single dose (chewed or dissolved) as soon as
  possible.
• ADD
• Nitrates, short acting, e.g.: isosorbide dinitrate, sublingual, 5 mg
  immediately as a single dose.
• May be repeated at 5-minute intervals for 3 or 4 doses.
• ADD
• Morphine 10 mg diluted with 10 mL of water for injection or sodium
  chloride 0.9%, slow IV (Doctor prescribed).
• Start with 5 mg; thereafter slowly increase by 1 mg/minute up to 10 mg.
• Can be repeated after 4–6 hours if necessary, for pain relief.
• Beware of hypotension.

Question 21

List the Initial management of unstable acute MI & STEMI

Answer 21

• Before transfer: cardiopulmonary resuscitation if necessary
• Oxygen 40% via facemask, if saturation < 94% or if in distress.
• Aspirin, oral, 150 mg as a single dose (chewed or dissolved) as soon as possible.
• AND
• Nitrates, short acting, e.g.: isosorbide dinitrate, sublingual, 5 mg immediately as a
  single dose.
• May be repeated at 5-minute intervals for 3 or 4 doses.
• AND
• Morphine 10 mg diluted with 10 mL of water for injection or sodium chloride 0.9%,
  slow IV (Doctor prescribed).
• Start with 5 mg; thereafter slowly increase by 1 mg/minute up to 10 mg.
• Can be repeated after 4–6 hours if necessary, for pain relief.
• Beware of hypotension.
• AND (if patient qualify)
• Thrombolytic: streptokinase OR if unavailable alteplase

Question 22

List the indications for thrombolytic therapy for acute MI and STEMI

Answer 22

For acute myocardial infarction with ST
elevation or left bundle branch block:
* maximal chest pain is ≤6 hours
* beyond 6 hours and chest pain, consult a
specialist
* >6 hours and no chest pain, manage with
anticoagulants
* if on-going ischaemic pain

Question 23

List the absolute contra-indications for thrombolytic therapy for acute MI and STEM

Answer 23

Absolute:
* streptokinase used within the last year, (not for alteplase)
* previous allergy,
* CVA within the last 3 months,
* history of recent major trauma,
* bleeding within the last month,
* aneurysms,
* brain or spinal surgery or head injury within the preceding
month, or recent (<3 weeks) major surgery,
* active bleeding or known bleeding disorder,
* aortic dissection.

Question 24

List the relative contra-indication for Thrombolytic therapy for acute MI and STEMI

Answer 24

Relative (consult specialist):
* refractory hypertension,
* warfarin therapy,
* recent retinal laser treatment,
* subclavian central venous catheter,
* pregnancy,
* TIA in the preceding 6 months,
* traumatic resuscitation.

Question 25

What to Note under Indications for thrombolytic therapy for acute MI and STEMI

Answer 25

Note: The mortality benefit of fibrinolysis is
highest when administered early after
symptom onset but is negligible if
administered to patients with symptom
durations exceeding 12 hours.

Question 26

Thrombolytic therapy for acute MI & STEMI
After administration, monitor continuously what and note

Answer 26

Pulse
* BP
* Respiration depth and rate (count for a full minute)
* ECG
* Note: defibrillator should always be readily available including during
transport

Question 27

When there is thrombus formation in setting of ACS what to use

Answer 27

Due to the role of thrombus formation in the setting of ACS, timely
and appropriate antithrombotic therapy is an important component
of optimal pharmacotherapy.

Question 28

Antithrombotic therapy consists of what?

Answer 28

Antithrombotic therapy consists of
* antiplatelet and
* anticoagulant therapy.

Question 29

explain the pathophysiologic process in arterial thrombosis

Answer 29

While platelets dominate the pathophysiologic process in arterial
thrombosis, the central role of thrombin in both platelet activation
and coagulation makes both types of therapy necessary in the acute
phase of treatment in a patient with ACS.

Question 30

List the antiplatelet treatment

Answer 30

Clopidogrel
Aspirin, oral, 150 mg stat, then as daily single dose, continued
indefinitely in the absence of contraindications

Question 31

Explain the action of antiplatelet treatment: aspirin

Answer 31

Provides its antiplatelet effect by acetylating a hydroxyl group of
serine 530 on the cyclooxygenase (COX) 1 enzyme on platelets and
thereby preventing the conversion of arachidonic acid into
prostaglandins, and eventually thromboxane A2.

Question 32

Activity of Thromboxane A2

Answer 32

Thromboxane A2 produces platelet activation as well as
vasoconstriction.