Lecture 42 Flashcards

Direct Acting Agonists

1
Q

Dobutamine

A
  • Beta 1 Selective agonist
  • Increases contractility and chronotropic (HR) effects): increases CO
  • Systolic BP in elevated
  • Diastolic BP and mean arterial pressure are unchanged
  • NO effects on dopamine receptors
  • Given IV, half life = 2 minutes
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2
Q

Dobutamine Uses

A
  1. Short term IV inotropic treatment in those with decompensated CHF and following heart surgery
    * *Only use for 48-72 hours due to desensitization with prolonged use**
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3
Q

Dobutamine Contraindications/Adverse Effects

A

Contraindication: Hypertrophic subaortic stenosis

Adverse Effects: Angina, palpitations, N/V, hypertension

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4
Q

Short Acting Beta 2 Agonists

A
  • Albuterol (Proventil, Ventolin)
  • Terbutaline (Brethaire)

Use to treat breakthrough symptoms and immediate prevention of exercise-induced bronchospasms

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5
Q

Long Acting Beta 2 Agonists

A
  • Salmeterol (Serevent) - onset 10-20 minutes
  • Formoterol (Foradil) - onset 1-3 minutes
  • Advair Diskus (Fluticasone/Salmeterol)

Use to treat moderate - severe, persistent asthma when symptoms aren’t controlled by corticosteroids alone

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6
Q

Beta 2 Agonists

A
  • Differ on selectivity and onset/durations
  • Relax/dilate smooth muscle in lungs, uterus, and vasculature of skeletal muscle
  • Stabilize mast cells (inhibit histamine and leukotriene release)
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7
Q

Beta 2 Agonist Uses

A
  1. Acute bronchospasm - in those with asthma and COPD
  2. Bronchospasm prophylaxis - prevention of exercise-induced bronchospasm
    - Inhibition of uterine contraction in premature labor (off label)
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8
Q

Metaproterenol

A
  • Alupent
  • Aerosol inhalation
  • Onset - 1-30 minutes, peaks at 1 hour, duration 4 hours
  • Treats acute bronchospasm in asthma/COPD
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9
Q

Terbutaline

A
  • Brethaire
  • Administered via tablet or SC
  • Used to reverse acute bronchospasm in asthma/COPD
  • Inhibits uterine contractions for 48-72 hours as well (off label use)
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10
Q

Terbutaline WARNING

A
  • Do not use in pregnant women to prevent or prolong preterm labor for more than 48-72 hours
  • Can cause serious, maternal heart problems and death
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11
Q

Albuterol/Levalbuterol

A
  • Albuterol = Proventil, Ventolin
  • Levalbuterol = Xopenex, R-isomer of Albuterol (s-isomer has no effect)
  • Combination: Duoneb or Combivent (Albuterol + Ipratropium)
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12
Q

Albuterol

A
  • Inhalation, tablets, solution
  • Used to treat acute bronchospasms in asthma
  • Also in breakthrough symptoms in asthmatics
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13
Q

Levalbuterol

A

-Prevents bronchospasms in those 6 years old and older with reversible, obstructive airway disease

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14
Q

Salmeterol

A
  • Serevent
  • Duration - 12 hours
  • Combination: Advair (Salmeterol + Fluticasone) - maintenance inhaler for COPD/asthma
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15
Q

Salmeterol Uses

A
  1. Maintain/prevent astham with concomitant corticosteroids
  2. Bronchospasm prophylaxis with COPD
  3. Prevent exercise-induced bronchospasm
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16
Q

Clenbuterol

A
  • Vet use only
  • B2 agonist
  • Increases lean body mass and activates lipases through B-receptors
  • Considered doping substance by most athletic organizations
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17
Q

Formoterol

A
  • Foridil
  • Selective B2 agonist
  • Quicker onset than Salmeterol with similar duration
  • Same uses as Salmeterol
18
Q

Salmeterol and Formoterol

A
  1. NOT indicated for acute asthma attacks or status asthmaticus
    * *Don’t take extra doses, use short acting B2 agonists for acute bronchospasms**
  2. NOT substitute for corticosteroids
  3. “Step Down Therapy” - D/C by reducing the dose by 25-50% every 3 months to the lowest dose possible
19
Q

LABA Black Box

A
  • Increase the risk of asthma-related deaths
  • Increase risk of asthma-related hospitalization
  • Use with concomitant use of long-term asthma control medications (inhaled corticosteroids)
  • Don’t use if controlled with corticosteroids
  • Pediatric/adolescents who need this drug, preferably prescribe combination with corticosteroid to increase adherence of both
20
Q

Beta 2 Agonist Contraindications

A
  • *Possible Beta 1 effects**
  • Harmful scale: IV > IM = SC > Oral > Inhalation
    1. Hypertension, cardiac arrhythmias, cardiac disease due to possible beta 1 activation
    2. Hyperthyroidism - increases number of beta receptors in heart, dose related B1
    3. Diabetes Mellitus - Beta agonists increase blood glucose
21
Q

Selective Beta 3 Agonist

A
  • Mirabegron (Myrbetriq)
  • Bladder relaxation of detrusor muscle
  • Increases bladder capacity
  • At usual doses: selective for B3
  • Adverse reaction: hypertension in 9-11%
  • Combine with antimuscarinic drug if symptoms persist
22
Q

Seletive Alpha-1 Agonist

A
  • Vasoconstrictors
  • Direct or indirect sympathetic effects
  • Used as decongestants and to increase BP
23
Q

Phenylephrine

A
  • Neosynephrine
  • Similar to epinephrine structurally
  • Alpha 1 agonist, potent vasoconstrictor
  • Tablet, liquid, sprays
  • Mainly used in combination with antihistamine, dextromethorphan, or APAP
  • Metabolized by MAO in liver/intestine
  • Used for nasal congestion from cold and allergies

Recent studies found that, when taken orally, doses as high as 40 mg were no more beneficial than a placebo

24
Q

Midodrine

A
  • Proamatine
  • Alpha 1 agonist
  • Oral
  • Used for severe postural hypotension (titrate)
  • Avoid near bedtime, can cause supine hypertension
  • Contraindication: heart disease, renal disease, urinary retention
  • Black box: increased supine BP
  • *Use in those who can’t tolerate fludrocortisone or to treat intermittent symptoms if non-drug measures fail (water and sodium)**
25
Q

Alpha 1 Agonist Contraindications

A
  1. Severe cardiac disease and arrhythmias
  2. During labor
  3. Hypertension
  4. Hyperthyroidism, especially if they have an indirect action that could release NE onto the heart
26
Q

Selective Alpha 2 Agonists

A
  • Anti-hypertensive effect - CNS activation on locus ceruleus/nucleus tractus solitarius
  • Central in origin: can’t cross BBB, can’t lower BP
  • Suppresses sympathetic NS activity, PNS predominates
  • Useful to treat anxiety, insomnia, pain, and opioid withdrawal (Clonidine patients ideally have all of this)
  • Rebound: rapid withdrawal can produce nervousness and anxiety and increase the BP
27
Q

Clonidine

A
  • Catapres
  • Epidural, oral, patch
  • Side effect = sedation
28
Q

Clonidine Uses

A
  1. Treat hypertension
  2. Withdrawal from opioids, ethanol, and nicotine side effects: decrease sympathetic outflow
  3. Treatment of severe pain in cancer patients; epidural produces analgesia (Duraclon - injection)
  4. Treat ADHD, especially in those with sleep disturbances
    - Treat symptoms of anxiety if mainly SNS in nature
29
Q

Clonidine ADHD Treatment

A
  • Clonidine ER (Kapvay) and Guanfacine (Intuniv)
  • Good alternatives for kids who can’t tolerate stimulants
  • May be added on to stimulant therapy as well
  • FDA approved to be monotherapy or add-on
  • Withdrawal symptom: rebound hypertension
30
Q

Guanfacine

A
  • Intuniv
  • More selective than Clonidine for alpha-2
  • Less frequency and severe rebound
  • Use to treat hypertension (moderate to severe)
31
Q

Guanabenz

A
  • Wytensin

- Treats moderate to severe hypertension

32
Q

Dexmedetomidine

A
  • Precedex
  • Alpha 2 agonist
  • May produce sedation and decrease anxiety
  • Half life 2.5 hours, used for 2-30 days and no incidence of rebound tachycardia/hypertension reported upon withdrawal (unlike clonidine)
33
Q

Precedex Uses

A
  1. Sedation of intubated and ventilated ICU patients
  2. Sedation of non-intubated patients prior and during surgical procedures
    * *Inhibits SNS and allows less opioids to be needed, doesn’t produce respiratory depression**
34
Q

Methyldopa

A
  • Aldomet
  • Oral and parenteral
  • Therapy for moderate to severe hypertension
  • Converted to alpha-methylNE
  • Stimulates CNS alpha-2 receptors
  • BOX WARNING - When used to HCT, not for initial hypertension therapy, need to titrate patients specifically
35
Q

Brimonidine

A
  • Alphagan
  • Ophthalmic solution
  • Treats increased IOP in open angle glaucoma or ocular hypertension
  • Decreases aqueous humor production and increases outflow via uveoscleral pathway (alpha 2 and prostaglandins open it)
  • 1000x more selective for alpha 2 than 1 (1 causes mydriasis which could further increase IOP)
36
Q

Combigan

A

Combination of Brimonidine + Timolol

37
Q

Apraclonidine

A
  • Iopidine
  • Alpha 2 agonist
  • Ophthalmic solution
  • Less CV side effects
  • Similar uses as brimonidine, shorter duration
38
Q

Tizanidine

A
  • Zanaflex
  • alpha 2 agonist
  • Decreases spasticity causes by MS or spinal injury
  • Corticospinal motor neurons transmit via glutamate in motor neurons of spinal cord, presynaptic alpha-2 receptors on these neurons inhibit the glutamate release
39
Q

Tramadol

A
  • Ultram
  • Oral analgesic
  • Affinity for mu receptor: 30%, blocks NE receptors: 70%
  • Increases NE in synapse which activates alpha 2 presynaptic receptors
  • Inhibits calcium uptake into the neuron and decreases glutamate release, decreases transmission of pain pathway
40
Q

Tramadol Contraindications

A
  1. Abrupt D/C - rebound hypertension, anxiety, nervousness
  2. Don’t use in those with heart or stroke disease, hypotensive effects may decrease perfusion and worsen ischemic conditions
41
Q

Tramadol Adverse Effects

A
  • Sedation
  • Headache
  • Fatigue
  • Confusion
  • N/V
  • Ejaculation dysfunction
  • Hypotension