Pharm 3 SE #2 Flashcards by Francis Malaj

What are some adverse effects/drug interactions of antimuscarinics?

Poor absorbtion, Dryness of mouth, urinary symptoms, Bitter metallic taste (ipratropium), nebulization with mask over eyes may precipitate acute glaucoma, Anticholinergic side effects in mod to severe renal function, additive interaction with other anticholinergics.

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Prototype SAMA

Ipratropium

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Prototype LAMA

Tiotropium

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Prototype SABA

Albuterol

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Prototype DPI LABA

Salmeterol

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Prototype Nebulized solution LABA

Formoterol

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Phosphodiesterase inhibitor, therapy must be individualized to achieve optimal responses and minimal side effects.

Theophylline - used for the treatment of asthma and COPD for decades. Currently, the role of theophylline is limited for these indications due to the introduction of inhaled bronchodilators and the potential for serious adverse reactions with xanthine derivatives. Theophylline is now considered as last-line or adjunct therapy for these indications. Theophylline has a narrow therapeutic range, and changes in dosing should only occur after a serum concentration is obtained.

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At low doses, this drug can cause nausea, irritability, insomnia, headache, vomiting. At high doses, it can cause ventricular arrhythmias, seizures

Theophylline

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This drug should not be given in patients with cirrhosis or patients who smoke cigarettes.

Theophylline

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What are the key points of bronchodilators?

Inhaled treatment is preferred, Long-acting bronchodilators are preferred, consider combo mechanisms, LAMA has a greater effect on exacerbation rates vs LABA, Theophylline not recommended unless other long-term tx are not an option.

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Does regular treatment of ICS improve disease progression or mortality?

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Are ICS as a monotherapy recommended?

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ICS should have the best effect if blood eosinophil count is what?

Blood eosinophil count > 300 cells/ul

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What is the holy trinity of COPD treatment that improves lung function, symptoms and health status and reduces exacerbation.

ICS + LABA + LAMA

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Do ICS put you at an increased risk of pneumonia?

Yes

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What should ICS be used in combination with for COPD?

Long-acting bronchodilators

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Name a LABA + ICS combo that is a DPI.

Fluticasone/Salmeterol (advair)

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Name a LABA +ICS combo that is a MDI

Budesonide/Formoterol (symbicort)

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Name a ICS + LAMA + LABA combo. DPI

Fluticasone, umeclidinium, vilanterol (Trelegy)

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This is a phosphodiesterase-4 inhibitor. Adverse effects ae nausea, reduced appetitie, abd pain, diarrhea, sleep disturbances, headache. You must monitor weight loss and depression.

Roflumilast (Daliresp)

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PDE-4 inhibitors must always be used in combination with what?

One long-acting bronchodilator

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These drugs can be used as anti-inflammatory drugs for COPD.

Azithromycin and Erythromycin

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What is the adverse effect of azithromycin?

Increased bacterial resistance, impaired hearing tests.

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What is the adverse effect of Erythromycin?

GI discomfort

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FEV1: 50-79% predicted

Moderate GOLD 2

FEV1: 30-49% predicted

Severe GOLD 3

What two vallidated questionnaires do we use to assess COPD?

COPD Assessment Test (CAT) | Modified British Medical Research Council (mMRC)

Which test only looks at dyspnea?

mMRC

Name the two groups that are mMRC 0-1 or CAT<10.

A and C

Name the two groups that are mMRC ≥2 CAT ≥ 10

B and D

Treatment for Group A COPD

Bronchodilator

Treatment for Group C COPD

LAMA

Treatment for Group B COPD

LABA or LAMA

Treatment for Group D COPD

LAMA, or LAMA+LABA, or ICS+LABA

What two COPD treatment groups are considered if there are 0 or 1 moderate exacerbations not leading to hospitalization?

Group A or B

What two COPD treatment groups are considered if there are ≥ 2 moderate exacerbations or ≥ 1 leading to hospitalization.

Group C or D

When treating Dyspnea, what is the next step if a LABA or a LAMA is ineffective?

Use both a LABA + LAMA together

When treating Dyspnea, what is next step if a LABA + ICS is ineffective?

Use the trio of LABA+LAMA+ICS

When treating Dyspnea, what should you do if the LABA+LAMA combo or the Trio is ineffective?

Consider switching inhaler device or molecules. | Investigate and treat other causes of dyspnea.

When treating Dyspnea, what should you do if you're using an ICS and the patient has pneumonia?

Consider de-escalation to just a LABA+LAMA combo

When treating Dyspnea exacerbations, when would you jump from a LABA or LAMA straight to a LABA +ICS instead of the LABA/LAMA combo?

If their blood eosinophil count is ≥ 300 and 2 moderate exacerbations or 1 hospitalization.

What is the most effective anti-inflammatory med class available for asthma?

ICS

Response to this drug therapy includes: symptoms improve in 1-2 weeks 4-8 max, FEV1 requires 2 mo for max improvement.

ICS

What may be a systemic adverse effect of ICS

Alterations in glucose metabolism.

What strategies reduce potential for adverse of events when using ICS?

``` Using a holding chamber Rinse mouth Using lowest dose possible Using in combination with LABAs Avoiding drugs that are CYP3A4 inhibitors like Ritonavir, ketoconazole ```

These drugs stimulate adenyl cyclase resulting in increased intracellular cyclic AMP which triggers bronchial smooth muscle relaxation. They selectively work on beta 2 receptors.

LABA

For Asthma, are LABA's appropriate as a monotherapy?

Salmeterol has a box warning of what?

Increased risk of asthma-related death.

What ICS LABA combos are there for asthma?

Fluticaslone/Salmeterol (Advair) Fluticasone/Vilanterol (Breo) Budesonide/Formoterol (Symbicort)

What are the main adverse effects of Leukotriene RREceptor Antagonist (LTRA)?

Nightmares and neuropsychiatric events.

What is the most effective medication for relief of acute bronchospasms?

SABA

What SABA uses frequency indicates inadequate asthma control?

using > 2 days/week.

These are used in treatment of asthma exacerbations and in treatment of impending episodes of severe asthma unresponsive to bronchodilator therapy.

Oral steroids

What are the monitoring intervals for asthma?

2-6 weeks, follow up 1-6 months, step-down therapy in 3 mo intervals.

What are 1st line agents for HTN

ACE/ARBS, Ca channel blockers, Thiazide diuretics

What are the criteria for diagnosing HTN?

2 or more properly measured BP readings taken 1-2 minutes apart and BP is elevated when measuring two or more visits spaced 1-4 weeks apart.

What is the 10-year risk of stroke or MI in an elevated 120-129/<80 BP and what is the recommendation?

N/A 10-year risk | Non-pharm, reassess in 3-6 mo.

What is the 10-year risk of a Stage 1 130-139/80-89? What is the recommendation?

<10% 10-year risk Non-pharm, reassess in 3-6 mo If ≥10% or clinical ASCVD then non-pharm +med and reassess in 1 month.

What is the 10-year risk and recommendation of a stage 2 ≥140/90?

N/A 10-year risk | Non-pharm + meds (2)

JNC8 BP goals for: | General population <60 years, Chronic kidney disease, ≥18 years, and Diabetes, ≥18 years.

<140/90mmHg

JNC8 BP goal for General population ≥60 years.

<150/90 mmHg

If the patients BP is ≥130/80 mmHg what other guidelines indicates use of meds.

If they also have a clinical CVD, a 10-year ASCVD risk ≥10% or if their BP is ≥140/90 mmHg

What are 2nd line HTN meds?

Loop diuretics, Potassium-sparing diuretics, Aldosterone antagonist diuretics, Beta blockers, alpha 1 blockers, Alpha agonist, Vasodilators.

For patients with BP >20/10 mmHg over their goal.

You can give two first-line agents of different classes except you can't combine ACE and ARBs.

What broad class of drugs should you consider to reduce blood volume (reduces CVP and CO)?

Diuretics

What broad class of drugs should you consider if you want to reduce cardiac output (Decrease HR, contractility, and stroke volume)

Beta blockers and Non-dihydropyridine calcium channel blockers.

Inhibit sodium chloride cotransporter in distal convoluted tubule in the kidney --> increased sodium and chloride excretion.

Thiazide diuretics

SE: hypokalemia*; metabolic alkalosis; hypotension; sun sensitivity; hyperglycemia; hypo-natremia, magnesemia, -phosphatemia; hypercalcemia SSE are: cardiac arrhythmias, SJS

Thiazide diuretics

Not appropriate for: patients with active gout; caution with history of gout; anuricpatients; less effective in patients with CrCl <30ml/min

Thiazide Diuretics

SE are: cough; hypotension; dizziness; headache; hyperkalemia.

ACE inhibitor

Not appropriate for pregnant patients and those with a hx of angioedema.

ACE inhibitors and ARBS

SE: Hypotension; dizziness; headache; hyperkalemia. SSE: Angioedema

ARBs

Ca channel blockers that are more selective for vascular cells; minimal direct cardiac effects.

Dihydropyridines - Amlodipine, nifedipine, felodipine

Ca channel blockers that are more selective for cardiac myocytes; less effects on systemic vasodilation.

Non-dihydropyridines - Diltiazem, verapamil

SE are: Hypotension, dizziness, peripheral edema*

Dihydropyridines like amlodipine

Effective as antihypertensive as well as anti-arrhthmics.

Non-dihydropyridines

Not appropriate for patients with heart failure*, bradycardia*, hypotension

Non-dihydropyridines

Side effects: Bronchospasm, bradycardia, hypotension, dizziness, fatigue, depression.

Beta blockers

Boxed warning: Abrupt cessation of therapy may lead to angina, myocardial infarction, death.

Beta blockers

BB's of choice for heart failure with a reduced ejection fraction.

Metoprolol succinate, carvedilol, and bisoprolol.

Inhibit sodium-potassium-chloride cotransporter in the thick ascending limb

Loop diuretics

Side effects: hypomagnesemia; hypokalemia; hyperuricemia; hypotension; metabolic alkalosis SSE: Ototoxicity, anemia, thrombocytopenia, SJS.

Loop diuretics

inhibit sodium channels in late distal convoluted tubule and collecting ducts. Used to prevent hypokalemia.

Potassium-sparing diuretics - Amiloride and triamterene.

SE: gynecomastia and erectile dysfunction.

Aldosterone antagonist diuretics - Spironolactone

Block the action of aldosterone at distal segment of the distal tubule; compete for the aldosterone-dependent sodium-potassium exchange site in distal tubule cells --> increased secretion of water and sodium.

Aldosterone antagonist diuretics - Spironolactone

Last line treatment for HTN, these act as vasodilators acting in the CNS to reduce sympathetic outflow from the CNS -- > decreased peripheral resistance, renal vascular resistance, heart rate and blood pressure.

Alapha-2 Agonists (clonidine, Methyldopa, Guanfacine)

This drug may be considered an add-on for resistant hypertension. Highly specific action on arterial vessels reduces vascular resistance and arterial pressure. Opening of K+ channels to cause smooth muscle hyperpolarization; inhibition of calcium release in smooth muscle; stimulates formation of nitric oxide to produce vasodilation. Has a SSE of lupus-like syndrome.

Hydralazine