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Drugs Flashcards

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1
Q

How does Combined Hormonal Contraception (CHC) work?

A

Inhibition of ovulation: Prevents the release of eggs from the ovaries.

Thickening of cervical mucus: Makes it harder for sperm to enter the uterus.

Endometrial changes: Makes the lining of the uterus less suitable for implantation of a fertilized egg.

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2
Q

What are the natural oestrogens used in hormone replacement therapy (HRT)?

A

Estradiol (oestradiol)

Estrone (oestrone)

Estriol (oestriol)

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3
Q

What is ethinylestradiol, and why is it commonly used in CHC?

A

Ethinylestradiol is a synthetic derivative of estradiol (natural oestrogen).

It is used in most CHC products because it has greater oral bioavailability than natural oestrogens, making it effective in lower doses.

It also has a longer duration of action compared to natural oestrogens.

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4
Q

What are some potential risks associated with ethinylestradiol?

A

Thromboembolic events (e.g., deep vein thrombosis, pulmonary embolism)

Increased blood pressure

Risk of stroke and heart attack, particularly in smokers or women over 35 years of age.

Breast cancer risk: Slightly elevated in long-term users.

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5
Q

How does the COC pill work?

A

Contains both oestrogen (usually ethinylestradiol) and a progestogen (e.g., levonorgestrel, desogestrel).

Taken daily for 21 days, followed by a 7-day pill-free or placebo break.

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6
Q

What are the common side effects of the COC pill?

A

Nausea

Headaches

Mood changes

Breast tenderness

Weight gain (in some cases)

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7
Q

What are the contraindications for COC use?

A

Active or history of thromboembolic disease (e.g., DVT, PE)

Uncontrolled hypertension

Severe liver disease

Breast cancer or hormone-sensitive cancer

Pregnancy

Smokers over 35 years of age

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8
Q

How does the combined transdermal patch work?

A

The patch releases both oestrogen and progestogen into the bloodstream through the skin.

It is worn on the skin for 7 days, with a new patch applied each week for 3 weeks followed by a 7-day patch-free break.

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9
Q

How does the combined vaginal ring work?

A

The ring is a flexible plastic ring that releases oestrogen and progestogen over a 3-week period.

It is inserted into the vagina and removed for a 1-week ring-free break.

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10
Q

What are the common side effects of the vaginal ring?

A

Vaginal irritation or discharge

Headache

Mood changes

Nausea

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11
Q

What are some common drugs that may interact with CHC and reduce its efficacy?

A

Antibiotics (e.g., rifampicin, rifabutin): Can reduce the effectiveness of CHC by inducing liver enzymes.

Anticonvulsants (e.g., phenytoin, carbamazepine): Increase liver metabolism of contraceptive hormones.

St. John’s Wort: Known to reduce the effectiveness of hormonal contraception.

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12
Q

What advice should a pharmacist give to a patient taking CHC and antibiotics?

A

Advise the patient to use additional contraception (e.g., condoms) while taking antibiotics and for 7 days after completing the course, depending on the antibiotic.

Most antibiotics (e.g., amoxicillin, penicillin, cephalosporins, doxycycline, clindamycin, etc.) do not reduce the efficacy of CHC.

The NICE guidelines (National Institute for Health and Care Excellence) and other clinical sources indicate that, although a theoretical risk exists for antibiotics altering gut flora and affecting hormone absorption, no significant evidence supports a clinically relevant interaction with these antibiotics.

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13
Q

What is the effect of smoking on CHC use?

A

Smoking increases the risk of thromboembolic events, especially in women over 35 years of age. It is advisable for women using CHC to avoid smoking or consider alternative methods of contraception.

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14
Q

What should a pharmacist monitor in patients on CHC?

A

Blood pressure: Because oestrogen can increase blood pressure.

Signs of venous thromboembolism (e.g., swelling, pain, shortness of breath).

Adverse reactions: Nausea, headache, or mood changes.

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15
Q

Can CHC be used in breastfeeding women?

A

Progestogen-only contraception is preferred during breastfeeding because oestrogen can affect milk production.

Combined methods may be used after 6 weeks postpartum, but only after assessing individual risks.

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16
Q

What should be done if a patient misses a COC pill?

A

If one pill is missed: Take it as soon as remembered and continue the pack. Use additional contraception for 7 days.

If two or more pills are missed: Follow the instructions on the pack and use additional contraception.

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17
Q

How do natural oestrogens differ from synthetic oestrogens like mestranol in terms of their profile?

A

Natural oestrogens are more bio-identical and typically have a better profile for hormone replacement therapy (HRT), being closer to the oestrogens naturally produced in the body.

Synthetic oestrogens (like mestranol) may have a higher risk of adverse effects, such as thromboembolism, due to different metabolic pathways.

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18
Q

What types of progestogen-only contraception are available?

A

Progestogen-only contraception includes:

Progestogen-only pill (POP)

Progestogen-only implant

Progestogen-only injectable

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19
Q

What are the key progestogens used in progestogen-only contraception?

A

Key progestogens include:

Progesterone (natural form)

Norethisterone (synthetic progestogen)

Desogestrel, Norgestimate, and Gestodene (synthetic derivatives of Norgestrel)

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20
Q

What are the characteristics of the newer synthetic progestogens like desogestrel, norgestimate, and gestodene?

A

Desogestrel, Norgestimate, and Gestodene are derivatives of norgestrel.

These progestogens are more selective for progestogen receptors and are often associated with less androgenic effects compared to older progestogens.

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21
Q

How does levonorgestrel compare to norgestrel in terms of potency?

A

Levonorgestrel is the active isomer of norgestrel and has twice the potency of norgestrel in terms of contraceptive effect.

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22
Q

What is the mechanism of action of progestogen-only contraception?

A

Progestogen-only contraception works by:

Thickening cervical mucus to prevent sperm from reaching the egg.

Inhibiting ovulation (primarily with progestogen-only pills containing desogestrel).

Thinning the endometrium to prevent implantation of a fertilized egg.

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23
Q

What are the potential side effects of norethisterone-containing contraception (e.g., POP, injectable)?

A

Common side effects include irregular bleeding, mood changes, headaches, acne, and changes in libido.

As a testosterone derivative, norethisterone can also cause androgenic side effects such as acne or increased facial hair in some users.

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24
Q

What are the key advantages of progestogen-only contraception (POP, implant, injectable)?

A

Suitable for women who cannot tolerate oestrogen (e.g., due to a history of blood clots, hypertension, or breastfeeding).

Effective in women with contraindications to oestrogen.

May reduce menstrual bleeding or even stop periods altogether (especially with the implant or injectable).

Long-acting reversible contraception (implant and injectable) with minimal user input.

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25
Which contraception is best with migraines?
Best Option for Migraines: Progestogen-only contraception (POP, implant, or injectable) is often the best option for individuals who suffer from migraines, especially those with aura (visual disturbances, etc.). Reason: These methods do not contain estrogen, which can potentially increase the risk of stroke in women with migraine with aura. Progestogen-only methods are safer because they do not interfere with blood clotting or vascular health in the same way that estrogen does.
26
What is the mechanism of action of norethisterone in delaying menstruation?
Norethisterone mimics progesterone, stabilizing the endometrial lining and preventing its shedding, thus delaying menstruation.
27
How soon before the expected period should norethisterone be started to delay menstruation?
Norethisterone should be started 5-7 days before the expected period. Norethisterone can be used for up to 10-14 days to delay periods
28
What is the most common side effect of norethisterone used to delay menstruation?
The most common side effect is irregular bleeding or spotting.
29
What is the typical dosage of norethisterone for period delay?
The typical dosage is 10 mg per day.
30
What should you do if you miss a dose of norethisterone?
Take the missed dose as soon as remembered and continue as normal.
31
Which of the following is a contraindication for using norethisterone to delay menstruation?
History of deep vein thrombosis (DVT) is a contraindication.
32
What off label drug can be used to delay periods?
Medroxyprogesterone acetate (Provera): Similar to norethisterone, this medication is sometimes used off-label to delay periods. The mechanism of action is similar in that it prevents the shedding of the uterine lining.
33
What is the mechanism of action of tranexamic acid?
It is an antifibrinolytic that inhibits plasminogen activation, reducing the breakdown of fibrin clots.
34
When is tranexamic acid typically taken during the menstrual cycle?
During menstruation only, usually for up to 4 days.
35
What are common side effects of tranexamic acid?
Nausea, vomiting, diarrhoea, and less commonly, visual disturbances or thromboembolic events.
36
What is a contraindication for using tranexamic acid?
Active thromboembolic disease or history of thrombosis e.g. DVT.
37
What class of drug is norethisterone?
A synthetic progestogen.
38
How does norethisterone help manage heavy menstrual bleeding?
It stabilizes the endometrium and suppresses menstruation by hormonal regulation.
39
How is norethisterone typically dosed for heavy menstrual bleeding?
5 mg three times daily for 10–14 days, starting on day 5 of the cycle.
40
What are common side effects of norethisterone?
Bloating, breast tenderness, mood changes, headaches, and breakthrough bleeding.
41
In which patients should norethisterone be used with caution?
Those with a history of thrombosis, liver disease, or hormone-sensitive cancers.
42
What is the contraindication for prescribing a PDE-5 inhibitor to a man with unstable angina?
PDE-5 inhibitors should not be prescribed to men with unstable angina or angina occurring during sexual intercourse.
43
Why should PDE-5 inhibitors not be prescribed alongside nitrates?
Concurrent use of PDE-5 inhibitors and nitrates can lead to severe, life-threatening hypotension.
44
What is the maximum recommended dose of sildenafil?
The maximum recommended dose of sildenafil is 100 mg, and it should not be taken more than once every 24 hours.
45
In which condition is sildenafil contraindicated?
Sildenafil is contraindicated in men with a history of non-arteritic anterior ischemic optic neuropathy (NAION).
46
What type of impairment requires dose adjustment when using tadalafil?
Tadalafil should be used with caution in cases of renal impairment (especially severe impairment) and hepatic impairment.
47
What should be avoided when using PDE-5 inhibitors regarding grapefruit?
Grapefruit should be avoided before taking PDE-5 inhibitors as it may increase plasma concentrations, especially with avanafil.
48
What is the dosing regimen for sildenafil in patients with renal impairment and creatinine clearance less than 30 mL/min?
In patients with renal impairment and creatinine clearance less than 30 mL/min, sildenafil should start at 25 mg and can be increased based on efficacy and tolerability.
49
What is the risk of combining PDE-5 inhibitors with alpha-blockers?
Combining PDE-5 inhibitors with alpha-blockers increases the risk of postural hypotension, as both are vasodilators.
50
What are common adverse effects of PDE-5 inhibitors?
Common adverse effects include headache, flushing, dyspepsia, nasal congestion, back pain, and myalgia (with tadalafil).
51
What is the primary mechanism of action of phosphodiesterase-5 (PDE-5) inhibitors like sildenafil?
Sildenafil inhibits PDE-5, which increases the concentration of cyclic guanosine monophosphate (cGMP) in the smooth muscle of the corpus cavernosum and pulmonary arteries. This leads to smooth muscle relaxation, vasodilation, and penile engorgement, aiding in erection during sexual stimulation.
52
Why should sildenafil be avoided in patients with severe hepatic or renal impairment?
In these patients, sildenafil metabolism and excretion are reduced, increasing the risk of adverse effects.
53
What serious drug interaction should be avoided with sildenafil?
Sildenafil should not be taken with nitrates or nicorandil as they both increase nitric oxide levels and cause marked vasodilatation, leading to a risk of cardiovascular collapse.
54
How can food affect the absorption of sildenafil?
The absorption of sildenafil is delayed if taken with food.
55
Why should sildenafil be prescribed with caution in patients taking other vasodilators like α-blockers or calcium channel blockers?
Both sildenafil and these vasodilators lower blood pressure, and when combined, they can increase the risk of hypotension.
56
What should you advise patients who are using recreational amyl nitrate (poppers) while taking sildenafil?
Warn them not to use amyl nitrate while on sildenafil, as the combination can cause severe cardiovascular effects, including collapse.
57
How should sildenafil be used for pulmonary hypertension?
Sildenafil for pulmonary hypertension (Revatio®) is prescribed regularly at a starting dose of 20 mg three times a day.
58
What monitoring is required for patients on sildenafil for pulmonary hypertension?
Regular monitoring with a specialist is needed for patients with pulmonary hypertension to assess treatment effectiveness and side effects.
59
What is the main indication for finerenone in CKD?
To reduce the risk of kidney disease progression and cardiovascular events in adults with chronic kidney disease associated with type 2 diabetes.
60
How does finerenone differ from spironolactone and eplerenone?
It is non-steroidal, more selective, and has a lower incidence of hormonal side effects and hyperkalemia.
61
What is the mechanism of action of finerenone in CKD?
It blocks mineralocorticoid receptors, reducing inflammation and fibrosis (the development of fibrous connective tissue as a reparative response to injury or damage) in kidneys and heart tissue.
62
What are the most important baseline labs before starting finerenone?
Serum potassium and estimated glomerular filtration rate (eGFR).
63
What is the main clinical use of sodium bicarbonate?
Treatment of metabolic acidosis, especially in renal failure, and management of certain drug overdoses (e.g., tricyclic antidepressants).
64
What is the mechanism of action of sodium bicarbonate?
It acts as an alkalinizing agent, neutralizing excess hydrogen ions and raising blood pH.
65
In which overdose situation is sodium bicarbonate particularly useful?
Tricyclic antidepressant (TCA) overdose to counter cardiac toxicity and QRS widening.
66
What are the key monitoring parameters when giving sodium bicarbonate IV?
Blood pH, bicarbonate levels, serum sodium, potassium, and arterial blood gases.
67
What are potential side effects of sodium bicarbonate?
Metabolic alkalosis, hypernatremia, hypokalemia, and fluid overload.
68
Why should sodium bicarbonate be used with caution in patients with heart failure?
It may cause sodium and fluid retention, exacerbating volume overload.
69
Why is sodium bicarbonate sometimes given orally in chronic kidney disease (CKD)?
To correct mild metabolic acidosis and potentially slow CKD progression.
70
What is a key contraindication to sodium bicarbonate therapy?
Metabolic or respiratory alkalosis.
71
Why do CKD patients often develop metabolic acidosis?
Because damaged kidneys can't remove excess acid or reabsorb enough bicarbonate, leading to acid buildup in the blood.
72
What is the chemical nature of sodium bicarbonate?
It is a base (alkali) that acts as a buffer to neutralize acid.
73
Why must sodium bicarbonate be used cautiously in CKD?
Because of the risk of fluid retention and worsening hypertension due to its sodium content.
74
What can metabolic acidosis cause?
1. Bone Disease (Osteodystrophy) Chronic acidosis leaches calcium and phosphate from bones to buffer acid. Leads to weakened bones, increased fracture risk, and osteomalacia. 2. Muscle Wasting (Proteolysis). Acidosis activates muscle breakdown pathways. 3. Fatigue and Weakness Low pH affects cellular metabolism and enzyme function. Patients may feel tired, weak, or short of breath. 4. Worsening of Cardiovascular Disease Acidosis can cause vascular inflammation, arrhythmias, and reduced cardiac contractility. May contribute to heart failure progression. 5. Electrolyte Imbalances Hyperkalemia (high potassium) is common, especially in kidney disease. Affects nerve and heart function, increasing the risk of arrhythmias. 6. Impaired Glucose Metabolism Metabolic acidosis reduces insulin sensitivity. May worsen insulin resistance and complicate diabetes management. 7. Mental Confusion or Reduced Consciousness Severe acidosis can impair brain function, leading to confusion, stupor, or even coma. 8. Increased Progression of CKD Metabolic acidosis is both a consequence and a driver of worsening chronic kidney disease. Promotes inflammation, fibrosis, and nephron loss.
75
Why are phosphate binders used in chronic kidney disease (CKD)?
To reduce phosphate absorption from the gut and manage hyperphosphatemia in CKD patients.
76
What is hyperphosphatemia, and why is it harmful?
Elevated phosphate in the blood; it can lead to vascular calcification, bone disease, and secondary hyperparathyroidism.
77
When should phosphate binders be taken?
With meals, to bind dietary phosphate in the gut.
78
Name two main types of phosphate binders.
Calcium-based and non-calcium-based (e.g., sevelamer, lanthanum).
79
What lab values should be monitored in patients on phosphate binders?
Serum phosphate, calcium, parathyroid hormone (PTH), and sometimes vitamin D.
80
What is the key advantage of sevelamer carbonate over calcium-based binders?
It does not raise serum calcium levels and may reduce vascular calcification risk.
81
What are common side effects of sevelamer carbonate?
GI issues such as nausea, bloating, and constipation.
82
Why might sevelamer be preferred in dialysis patients?
Because of its lower risk of hypercalcemia and cardiovascular calcification.
83
What are the two main indications for alpha-blockers?
First-line treatment for benign prostatic hyperplasia (BPH) when lifestyle changes fail. Add-on treatment for resistant hypertension.
84
What is the mechanism of action of alpha-blockers?
They selectively block α1-adrenoceptors, leading to relaxation of smooth muscle in blood vessels and the urinary tract, causing vasodilation and reduced bladder outflow resistance.
85
What are the main adverse effects of alpha-blockers?
Postural hypotension Dizziness Syncope - fainting (Especially after the first dose)
86
Why should alpha-blockers be avoided in certain patients?
They should not be used in patients with existing postural hypotension.
87
What interaction should you watch for when starting an alpha-blocker in a patient on a β-blocker?
β-blockers blunt reflex tachycardia, increasing the risk of first-dose hypotension when starting an alpha-blocker.
88
What are the most commonly prescribed alpha-blockers in the UK?
Doxazosin and tamsulosin.
89
Which alpha-blocker is licensed for both BPH and hypertension?
Doxazosin.
90
What is the initial dose of doxazosin, and how is it adjusted?
Start at 1 mg daily, increase at 1–2 week intervals based on response. Best to take at bedtime, to reduce the risk of first-dose postural hypotension.
91
What is the standard dose of tamsulosin, and what is it licensed for?
400 micrograms daily, licensed for BPH only.
92
What is the mechanism of action of 5-alpha reductase inhibitors?
They inhibit the enzyme 5-alpha reductase, which converts testosterone to dihydrotestosterone (DHT). It leads to reduced prostate volume and decreased androgenic stimulation of hair follicles.
93
Name two commonly used 5-alpha reductase inhibitors.
Finasteride and dutasteride.
94
What are the primary clinical indications for 5-alpha reductase inhibitors?
Benign prostatic hyperplasia (BPH) and androgenetic alopecia (male pattern baldness).
95
What are common side effects of 5-alpha reductase inhibitors?
Decreased libido, erectile dysfunction, ejaculatory dysfunction, and gynecomastia.
96
How long does it typically take for 5-alpha reductase inhibitors to have a clinical effect on BPH?
Several months (usually 3–6 months).
97
Why should women, especially those who are pregnant or may become pregnant, avoid handling crushed or broken 5-alpha reductase inhibitor tablets?
Because of the risk of absorption and potential harm to a male fetus (due to interference with DHT-dependent development).
98
When should antimuscarinics be prescribed for urge incontinence?
Only after an adequate trial of bladder retraining.
99
How do antimuscarinic drugs help in overactive bladder?
They competitively inhibit acetylcholine at muscarinic receptors, promoting bladder relaxation and increasing capacity.
100
Name three antimuscarinics commonly used for overactive bladder.
Oxybutynin, tolterodine, and solifenacin. First line treatment - Immediate-release oxybutynin.
101
What are very common side effects of antimuscarinics?
Dry mouth, tachycardia, constipation, and blurred vision.
102
What genitourinary complication can antimuscarinics cause, especially in patients with obstruction?
Urinary retention.
103
Why should antimuscarinics be used cautiously in elderly patients or those with dementia?
Due to the risk of drowsiness and confusion.
104
Why are antimuscarinics used cautiously in patients at risk of angle-closure glaucoma?
They can precipitate a rise in intraocular pressure.
105
What cardiac risk must be considered before prescribing antimuscarinics?
Risk of arrhythmias in patients with significant cardiac disease.
106
How does mirabegron work to relieve overactive bladder symptoms?
As a beta-3 adrenergic agonists it stimulates β₃-adrenoceptors in the bladder detrusor muscle, promoting relaxation during the storage phase.
107
What is the primary indication for mirabegron?
Treatment of overactive bladder with symptoms of urgency, increased urinary frequency, and urge incontinence.
108
What effect does β₃ stimulation have on bladder function?
Increases bladder capacity and reduces urgency and frequency.
109
What is a notable cardiovascular side effect of mirabegron?
Hypertension.
110
What are other potential side effects of mirabegron?
Tachycardia, urinary tract infections, headache, and nasopharyngitis.
111
What is the usual starting dose of mirabegron for adults?
25 mg once daily, which may be increased to 50 mg if tolerated.
112
What is the primary action of desmopressin in the treatment of enuresis or urinary incontinence?
It reduces urine production by mimicking antidiuretic hormone (ADH/vasopressin), promoting water reabsorption in the kidneys.
113
What adult urinary symptom may desmopressin also be used to treat?
Nocturia, particularly in women with troublesome night-time urination.
114
What is a serious risk associated with desmopressin therapy?
Hyponatraemia (low sodium), due to water retention. Symptoms include headache, nausea, confusion, and seizures.
115
Which EHC can be used in breast feeding?
Levonorgestrel. NOT ellaone - is still present in milk for a week.
116
How long should progesterone containing drugs be paused after taking ellaone?
They should not be started for 5 days afterwards - use barrier method until next period.

Genito-urinary system (13 decks)

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