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Pharm 1 > Adrenergics/Anti-Adrenergics > Flashcards

Adrenergics/Anti-Adrenergics Flashcards

1
Q

Indirect Acting Sympatho-mimetics

A

Cocaine

Tricyclic Anti-depressants (TCAs)

Amphetamines

Non-amphetamines

Atomoxetine

Modafinil

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2
Q

Cocaine and Tricyclic Anti-Depressants (TCAs)

A

Inhibit reuptake NE transporter (NET) in various locations (intentionally vs. unintentionally)

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3
Q

Amphetamines

A

Central Stimulant for ADHD

Centrally inhibit NET to increase attentiveness
-can also release stored monogamies

Amplification of SANS effects via increased monoamine receptor activation

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4
Q

Cocaine

A

Centrally:
Stimulate pre-synaptic NE release + inhibit NET +inhibit reuptake of domaine (DA) and serotonin (5HT)

Peripherally:
-stimulate pre-synaptic NE release and inhibits neuronal reuptake of both NE and E

Topically:
-Decreased nerve permeability to sodium (local anesthetic)

Therapeutic Use:

  • Topical Local anesthetic (sodium channel inhibitor)
  • seen primarily in the operating room

Illicit Use

  • stimulating effect->robust SANS activation with mild local anesthetic effects (depending on route of admin)
  • vasoconstriction: increased alertness: enhanced reward
  • no reversal agents
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5
Q

Amphetamine based stimulant

A

MOA: Promote release of NE primarily and DA (at high dose) from pre-synaptic storage into synapse
-also blocks NE/DA reuptake—>less significant effect

Uses:
ADHD, obesity, narcolepsy, binge eating

ADRs:
Increased SBP/DBP, tachyardia, lost/reduced appetite, weight loss, dry mouth, constipation, teeth grinding, abdominal pain, insomnia,
-cautious uses in Tourette’s - may exacerbate tics
-cautious use in cardiac compromise -tachycardia
-growth inhibition in children ?

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6
Q

Non-Amphetamines based Stimulants

A

MOA: Similar effect/use of amphetamines but mediated primarily by DA reuptake (less NE effects)

Similar ADRs but generally less pronounced (especially cardiac)

Methylphenidate (Ritalin) and Dexmethylphenidate

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7
Q

Atomexetine

A

Thought to involve NET reuptake inhibition

Non stimulant for treatment of ADHD

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8
Q

Modafinil

A

Increase NE/DA/5HT/Glu

Decreases GABA

Uses: narcolepsy, circadian rhythm disturbances

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9
Q

Indirect Acting Sympatholytics

A

Anti-adrenergic without directly blocking the receptors
-not commonly used anymore

Metyrosine and Reserpine

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10
Q

Metyrosine

A

Inhibits tyrosine hydroxylase (rate-limiting step in catecholamine synthesis) in an effort to decrease excess production/activity

Benefit seen in pheochromocytoma

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11
Q

Reserpine

A
  • Inhibits VMAT, reuptaken monoamines metabolized by MOA

- Anti-hypertensive effect (drug no longer used to hypertension given safer alternatives)

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12
Q

Selective Alpha-1 Agonists

A

Midodrine

Phenylephrine

Pseudoephedrine

Oxymetazoline

Naphazoline

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13
Q

Midodrine

A

Treats Orthostatic Hypotension

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14
Q

Phenylephrine

A

Cough cold

IV vasopressor

Eye drops

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15
Q

Pseudoephedrine

A

Decongestant for cough and cold

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16
Q

Oxymetazoline (Afrin)

A

Nasal Spray

Rhinitis Medicamentosa:

  • cannot use Afrin for more than 3 days, shrinks the nasal mucous
  • become dependent
  • leads to rebound congestion
17
Q

Alpha-1 Subtypes

A

1A: prostrate smooth muscle contraction

1B/1D: vascular smooth muscle contraction (blood vessels)
-1D: bladder neck

Antagonize 1A/1D=BPH relief (Benign Prostrate Hypertrophy)

  • less pressure on urethra
  • increased urinary flow
18
Q

Selective Alpha-1 Antagonists

A

Prazosin

Doxazosin ; Terazosin

Tamsulosin ; Alfuzosin

Silodosin

ADRs:

  • erectile dysfunction and abnormal ejaculation
  • dizziness/syncope, hypotension, reflex tachycardia for prazosin, doxazosin, Terazosin (less selective)
  • first dose phenomenon
19
Q

Prazosin

A

Use primarily in PTSD nightmares

20
Q

Doxazosin and Terazosin

A

Block all alpha-1 subtypes —>can use for BPH and or for HTN

21
Q

Tamsulosin and Alfuzosin

A

For treatment of BPH

More selective for alpha-1A receptors on prostate/urethra

Less cardiac effect
May want to use them in people with BP problems

22
Q

Silodosin

A

More selective for alpha-1A

Treatment for BPH

Least hypotensive

Less cardiac effect

23
Q

Selective Alpha 2 Agonists

A

Clonodine

Tizanidne

Guanfacine

Dexmedetomidine

Brimonidine

Apraclondine

Methyldopa

24
Q

Clonidine and Tizanidine

A

HTN

ADHD

Withdrawal

Muscle spasticity (t»c)

25
Q

Guanfacine

A

ADHD in Pediatrics

Older drug for HTN

26
Q

Dexmedetomidine

A

IV sedative with Sympatholytic/analgesic properties

27
Q

Brimonidine and Apraclonidine

A

Eye drops for glaucoma

Less aqueous humor production

28
Q

Methyldopa

A

Favorable agent for HTN pregnancy

29
Q

Non Selective Alpha Antagonists

A

Vasodilation while increasing cardiac output
-benefit seen in diagnosis/treatment of pheochromocytoma

Phenoxybenzamine (oral) or Phentolamine (IV/IM)

  • Phentolamine is paranteral and has shorter duration of action—>more inpatient uses
  • treatment of extravasation (potential dermal necrosis due to extensive use) from IV alpha-1 agonists=phentolamine can treat this

ADRs:
-Nasal Congestion, myosis(constriction of the pupal), orthostatic hypotension

30
Q

Selective Beta-1 Agonist

A

Dobutamine

  • positive inotropic effects»> chronotropic effects
  • IV; requires dose titration to desired effect

Therapeutic use (short-term)

  • cardiogenic shock; septic shock
  • acute congestive HF
31
Q

Selective Beta-1 Antagonists

A 
Metoprolol succinate 
Atenolol 
Nebivolol**
Bisoprolol **
Acebutolol 
Betaxolol 
Esmosol
  • At high doses, may become non-selective
  • *generally maintain selectivity at higher doses
32
Q

Selective Beta 2 Agonists

A

SABA: short acting
-albuterol and levalbuterol

LABA: long acting

  • formoterol, salmeterol, olodaterol, aformoterol, indacaterol
  • Terbutaline (oral tablets/parenteral)

Local administration ideal
PK differences between agents
Selective for beta-2 receptors» beta-1 receptors

33
Q

Non-selective Beta Agonists

A

Isoproterenol

  • primarily used for beta-1 effect (positive inotrope)
  • used largely replaced by dobutamine

Metaproterenol

  • primarily used for beta-2 effect
  • asthma/COPD, bronchospasm
34
Q

Non-selective Beta Antagonists

A

Nadolol
Propranolol

Carteolol, Timolol, Levobunolol, Metipranolol->ophthalmic

Sotalol
Prindolol

Therapeutic Uses:

  • Gluacoma; ocular hypertension (ophthalmic)
  • Migraine Prophylaxias; tremors; stage fright (propranolol)
  • Hypertension; atrial fibrillation; arrhythmias
  • Portal hypertension; esophageal varicose, bleeding prophylaxis (nadalol)
  • decrease portal vein pressure, decrease blood flow
35
Q

B-3 Receptor

A

Primarily theorized actions include lipolysis in adipose tissue and thermogenesis in skeletal muscle

Receptors found in gallbladder, heart, colon, CNS, brown adipose tissue and BLADDER

Expressed in DETRUSOR MUSCLE OF BLADDER
ACTIVATION results in RELAXATION of detrusor muscle

36
Q

Selective Beta 3 Agonist

A

MIRABEGRON

On the DETRUSOR muscle

37
Q

MIRABEGRON -uses

A

Used for symptoms of overactive bladder (OAB), urinary incompetence, urgency and frequency

Increased bladder capacity during storage phase

38
Q

Mirabegron ADRs

A

BP elevations

Tachycardia

  • mostly due to losing selectivity at higher doses
  • it is an alternative to anti-muscarinics for OAB

Pharm 1 (4 decks)

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