Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

PHARM > ANS Sympathetic Drugs > Flashcards

ANS Sympathetic Drugs Flashcards

1
Q

Norepinephrine

(Levarterenol)

A
  • Agent Type: Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Hypotension, shock (DOC, increasing in use), considered pressor agent (↑ BP).
  • Actions: Full agonist all receptors: α / β1 β2 β3 (weakest), neuronal, non-circulating, substrate for MAO & COMT. Does not cross BBB. Neuronal uptake inhibition →↑ effect (ie, c TCA, cocaine, atomoxetine).
  • CV:↑BP c reflex bradycardia. NE c atropine →↑BP c ↑HR
  • Notes: Short duration due to rapid metabolism. Given IV, IM, SC, not oral.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Epinephrine

(generic)

A
  • Agent Type: Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Anaphylaxis (DOC, allergic reactions), cardiogenic shock, cardiac arrest, glaucoma (↑outflow), severe bronchospasm. Not used for HF (↑O2 demand). Hypotension, ↑Shock, Pressor Agent
  • Actions: Full agonist all receptors: α / β1 β2 β3 (weakest), released from adrenal medulla, circulates, substrate for MAO & COMT. Does not cross BBB. Neuronal uptake inhibition →↑ effect (ie with TCA, cocaine).
  • Caution: Elderly, HTN, CV disease
  • CV: ↑ BP c ↑HR. EPI reversal (+α-blocker) →↓BP c ↑HR
  • Notes: Not oral.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Dopamine

(Intropin)

A
  • Agent Type: Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Shock syndrome (common use, ie. sepsis, Hi dose), acute HF (moderate dose). Can ↑ renal perfusion (D1-R).
  • Action: Full agonist all D-receptors, β1 (moderate dose), α1 (hi dose) , precursor to NE, substrate for MAO & COMT. NE/EPI precursor. Does not cross BBB.
  • Adverse: arrhythmias
  • Notes: Short duration. Not oral
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Pramiprexole, Bromocriptine

A
  • Agent Type: Adrenoceptor Agonists- Dopamine
  • Therapeutic Use (↑↓ Use): Parkinson’s D, hyperprolactinemia (Bromo), restless leg S. (Prami).
  • Action: D-Agonists, Prami (some D3-sel)
  • Adverse: Hallucinations, drowsiness
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Fenoldopam

(Corlopam)

A
  • Agent Type: Adrenoceptor Agonists- Dopamine
  • Therapeutic Use (↑↓ Use): HTN crisis (Acute HTN), renal failure.
  • Action: Dopamine D1A-Receptor Agonist (activates AC, ↑cAMP)
  • Adverse: Tachycardia, ↑ocular pressure, can ↓serum K
  • Notes: Used short-term by IV infusion
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Isoproterenol

(Isuprel)

A
  • Agent Type: β-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Heart block (cardiac stimulant),asthma (rarely, many adverse effects)
  • Action: Full agonist all β receptors (activates AC, ↑cAMP), substrate for COMT but poor for MAO, doesn’t cross BBB.
  • Adverse: Tachycardia, palpitations, angina
  • CV: Decrease BP c tachycardia (direct & reflex).
  • Notes: synthetic- not endogenous. Longer duration than NE or EPI but still short duration.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Phenylephrine

(Neosynephrine)

Methoxamine

(Vasoxyl)

A
  • Agent Type: α1-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Nasal decongestant, hypotension considered pressor agent, glaucoma (↑outflow).
  • Action: Full agonist α1-receptors, little or no β-activity, activate PLC, ↑Ca ↑IP3.
  • Note: Not commonly used for hypotension
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Clonidine

(Catapres)

Guanfacine

(Tenex)

A
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Hypertension (CNS to
    ↓ sympathetic outflow), opioid withdrawal (↓severity)
  • Action: α2-agonists (inhibit AC, ↓cAMP), inhibits NE release, cross BBB.
  • Adverse: Dry mouth, sedation, impotence, rebound HTN, bradycardia.
  • Note: Need to discontinue gradually to prevent rebound HTN.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

α-Methyl Dopa

(Aldomet)

A
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Hypertension (CNS, ↓outflow)
  • Action: Prodrug → metabolizd to α-methyl-NE (α2-agonist (↓cAMP), inhibits NE release.
  • Note: Very good safety profile as anti-HTN during pregnancy
  • Adverse: Sedation, bradycardia , may cause positive
    direct Coombs test (RBC destruction), liver disease
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Dexmedetomidine

(Precedex)

A
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Premed surgical sedation
  • Action: Alpha2-agonist (inhibits AC, ↓cAMP), ↓NE release, crosses BBB.
  • Adverse: Hypotension, ↓HR (may cause sinus arrest)
  • Note: Little respiratory depression. ↑use
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Tizanidine

(Zanaflex)

A
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Short-term muscle spasticity (ie. whiplash), multiple sclerosis
  • Action: Alpha2-agonist (inhibits AC, ↓cAMP), inhibits NE release, crosses BBB. CYP1A2 substrate
  • Adverse: Sedation, hypotension bradycardia, dry mouth.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Dobutamine

(Dobutrex)

A
  • Agent Type: β-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Acute heart failure/ CHF (
  • Action: Profile of β1 agonist, Activate AC (↑cAMP), Substrate for COMT & MAO. Substrate for CYP3A4 metabolism.
  • Adverse: Arrhythmias, tolerance. don’t confuse c DA.
  • Notes: 4 isomers
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Albuterol (Proventil, Ventolin)

  • *Metaproterenol** (Alupent, Metaprel)
  • *Terbutaline** (Brethine, Brethaire)
  • *Ritodrine** (Yutopar)
  • *Salmeterol (LABA)** (Serevent, Diskus)
A
  • Agent Type: β2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Asthma, Bronchospasm (rescue inhaler), COPD, Premature labor (Ritodrine)
  • Action: β2-agonists, (activate AC, ↑cAMP), causes bronchodilation, relax uterus. Albuterol is short-acting but not substrate for COMT or MAO.
  • Action 2: Long-acting β2-agonists (LABAs) are available for chronic treatment ie. salmeterol, formoterol, arformoterol [-terol]. Have ↑risk respiratory death & severe attacks.
  • Adverse: Tachycardia, tremor, restlessness
  • Notes: Although Terbutaline is not FDA approved for premature labor, it is commonly used.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Ephedrine

(Vatronol, Efedron)

A
  • Agent Type: Indirect Sympathomimetic Amine
  • Therapeutic Use (↑↓ Use): Nasal Decongestant, Red Eyes, orthostatic hypotension, appetite suppression
  • Action: Causes displacement of NE/DA & direct α- & β-receptor agonist. Can cross BBB to cause CNS
    stimulation. Enhanced effect c MAOI.
  • Adverse: Restlessness, tremor, insomnia, HTN, ↑HR
  • Notes: OTC
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Tyramine (Amino-acid)

A
  • Agent Type: Indirect Sympathomimetic Amine
  • Therapeutic Use (↑↓ Use): None, AA found in various foods (rich in aged cheese, red wine, liver, vegemite).
  • Action: Can cause a HTN crisis (↑BP, ↑HR) in pts receiving MAOI therapy (gut MAOA is important).
  • MAOs: Problem c non-selective MAO inhibitors (tranylcypromine) or MAOA selective (clorgyline) but not MAOB selective (selegiline) inhibitors.
  • Note: MAOA or non-selective MAO inhibitors used for
    depression treatment. MAOB selective inhibitors used for Parkinson’s D.
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

L-Dopa/ Carbidopa

(Dopar, Larodopa)

A
  • Agent Type: Neurotransmitter Precursor
  • Therapeutic Use (↑↓ Use): Parkinson’s D. (assoc. c loss of dopaminergic fxn in midbrain, results in tremor, rigidity, bradykinesia & postural instability).
  • Action: L-dopa crosses BBB converted to dopamine.
  • Adverse: Dyskinesias (jerky, involuntary movement), vomiting & nausea (reduced c Carbidopa)
  • Notes: Given c Carbidopa (inhibits peripheral decarboxylation, doesn’t cross BBB). L-dopa effectiveness dec. after 4-5 yrs & a dopamine agonist (ie. pramiprexole) is added to pharmacotherapy regimen. Next is usually addition of a MAOB inhibitor..
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

Phenoxybenzamine

(Dibenzyline)

A
  • Agent Type: α-Adrenoreceptor Antagonist
  • Therapeutic Use (↑↓ Use): Acute & chronic
    pheochromocytoma, HTN crisis.
  • Action: Irreversible α-receptor antagonist (slight α1 over α2 selectivity, x5).
  • Adverse: Orthostatic (postural) hypotension, reflex ↑HR → arrhythmia, nasal congestion.
  • Both CV: ↓BP c reflex tachycardia. CV: EPI reversal (+α-blocker) → ↓BP c ↑HR
  • Notes: Can inhibit M-receptors, histamine, serotonin & neuronal uptake, Impotence
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Phentolamine

(Tolazoline)

A
  • Agent Type: α-Adrenoreceptor Antagonist
  • Therapeutic Use (↑↓ Use): HT crisis, pheochromocytoma
  • Action: Non-selective, competitive α-receptor blocker. Block of pre-synaptic α2-receptors can ↑NE release.
  • Adverse: Orthostatic (postural) hypotension, reflex ↑HR → arrhythmia, nasal congestion.
  • Both CV: ↓BP c reflex tachycardia. CV: EPI reversal (+α-blocker) → ↓BP c ↑HR
  • Notes: low use
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

[-zosin]

  • *Prazosin** (Minipress)
  • *Terazosin** (Hytrin)
  • *Doxazosin** (Cardura)
  • *Tamsulosin (α1A-)** (Flomax)
A
  • Agent Type: α1-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): Benign prostatic hyperplasia (BPH), HTN, HTN crisis, Raynaud’s D.
  • Action: Selective, competitive α1-receptor blockers. Presynaptic α2-receptors unaffected → no reflex ↑HR (since α2-receptors operational). Tamsulosin α1A-selective.
  • Contra-indication: c PDE5 inhibitors ie Sildenafil (marked ↓BP)
  • Adverse: Orthostatic (postural) hypotension, nasal
    congestion.
  • Both CV: ↓BP s reflex tachycardia. EPI reversal (+α-blocker) → ↓BP c ↑HR
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

Mirtazapine (Mirtaz, Zispin)

Yohimbine (OTC)

A
  • Agent Type: α2-Adrenoceptor Antagonists
  • Mirtazapine: competitive α2-receptor blocker. Used in depression treatment ie. PTSD. Can ↑appetite, ↑5-HT release (CNS). Adverse: sedation
  • Yohimbine: No FDA approved use. OTC for sexual
    dysfunction, impotence. In vet medicine, yohimbine is used to reverse xylazine action (α2- agonist, used in vet. medicine for anesthesia, analgesia, sedation)
  • Alkaloid, competitive α2-receptor blocker. May enhance effects of MAO inhibitors.
  • Adverse: HTN, tachycardia, insomnia, dizziness, anxiety, tremor
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

β-Antagonists [-olol]

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, angina, arrhythmias (SVT), HF (Metoplolol, Carvedilol), tremor, migraine, post-MI, mild hyperthyroidism (propranolol only), panic attack, stage fright (stress)
  • Action: β1 Selective (A-M), β Non-Selective (N-Z)
  • Adverse: Effects enhanced in elderly but clinical effectiveness is ↓ in elderly or Afro-Americans, fatigue, dizziness, ↓ myocardial reserve, cardiac depression, worsen asthma (block of bronchial β2-ARs, less c β1-ARs or those c ISA), peripheral vascular insufficiency (may precipitate/worsen Raynand’s D.), Diabetes (mask symptoms, hepatic β2 → ↓ recovery, less c β1-ARs or those c ISA), CNS (nightmares, mental depression, insomnia), withdrawal syndrome (supersensitivity, rebound HT, less with ISA).
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Propranolol

(Indreal)

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, angina, arrhythmias (SVT), tremor, migraine, mild hyperthyroidism, panic attack, stage fright (stress), MI
  • Action: Non-Selective β-AR Antagonist, MSA (Membrane Stabilizing Activity) but NO Intrinsic Sympathomimetic Activity (ISA)
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Pindolol

(Visken)

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, Angina
  • Action: Non-Selective β-AR Antagonist, MSA (Membrane Stabilizing Activity), Intrinsic Sympathomimetic Activity (ISA)
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Timolol

(Blocadren)

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): Glaucoma (↓ Secretion), HTN, MI (Angina, Arrythmias)
  • Action: Non-Selective β-AR Antagonist, MSA (Membrane Stabilizing Activity), NO Intrinsic Sympathomimetic Activity (ISA), NO LA (Local Anaesthetic) Action.
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Metoprolol

(Lopressor)

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, Angina, Arrythmias (SVT Common), MI, Heart Failure (HF)
  • Action: β1-Selective Antagonist, MSA (Membrane Stabilizing Activity), NO Intrinsic Sympathomimetic Activity (ISA), Local Anaesthetic Action.
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Atenolol

(Tenormin)

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, Angina, Arrythmias, MI
  • Action: β1-Selective Antagonist, NO Intrinsic Sympathomimetic Activity (ISA), NO Local Anaesthetic Action.
  • Notes: Low Lipid Solubility (ie, CNS Action), Contraindication- Pregnant
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

Nebivolol

(Bystolic, Nebicip)

A
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN (newest β-blocker)
  • Action: β1-Selective Antagonist (at doses NO Intrinsic Sympathomimetic Activity (ISA), NO Local Anaesthetic Action.
  • Notes: Low Lipid Solubility (ie, CNS Action)
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

Esmolol

(Brevablock)

A
  • Agent Type: β1-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): Arrythmias, [angina]
  • Action: β1-Selective Antagonist, NO Intrinsic Sympathomimetic Activity (ISA), NO Local Anaesthetic Action.
  • Notes: Very short acting (10 min), used for arrythmias that arise during surgery.
  • Adverse: See β-antagonist Slide
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

Carvedilol (Coreg)

Labetalol (Normadyne)

A
  • Agent Type: α/β-Adrenoceptor Antagonists
  • Carvedilol
    • Therapeutic Use (↑↓ Use): Heart failure (common), HTN
    • Action: α/β-Selective Antagonist, NO MSA (LA), NO Partial Agonist (ISA).
  • Labetalol
    • Therapeutic Use (↑↓ Use): Angina, HTN crisis, HTN
    • Action: α/β-Selective Antagonist, MSA (LA) & partial agonist activity (ISA).
  • Adverse: Bronchoconstriction, asthma, worsen diabetes, supersensitivity, insomnia, depression, ↓HR, ↓BP, sexual dysfunction, fasting hypoglycemia.
  • CV Acute: ↓BP & ↓ HR, ↓CO
30
Q

Cocaine

(generic)

A
  • Agent Type: Indirect Sympathomimetics (Inhibit neuronal uptake)
  • Therapeutic Use (↑↓ Use): Local anesthetic, high drug abuse
  • Action: CNS stimulation, euphoria. LA-action (Na-channel block)
  • Adverse: HTN, myocardial ischemia, coronary spasm, arrhythmia
  • Notes: Inhibition of neuronal uptake (Uptake, 70-80% NE removal) to enhance NE effect. High lipid solubility.
  • Best Effect: Amphetamine Before Cocaine (ABC).
31
Q

Atomoxetine

(Strattera)

A
  • Agent Type: Indirect Sympathomimetics (Inhibit neuronal uptake)
  • Therapeutic Use (↑↓ Use): ADHD, considered as non-stimulant therapy
  • Action: Metabolized by CYP2D6.
  • Adverse: Arrhythmia, suicide tendency, myocardial
    ischemia, liver injury, agitation, panic attacks, insomnia.
  • Notes: Has less abuse potential than amphetamines (Ritalin, Methylphenidate).
32
Q
  • *Imipramine** (Tofrani)
  • *Amitriptyline** (Elavil)
A
  • Agent Type: Tricyclic antidepressants (TCAs)
    (Inhibit neuronal uptake)
  • Therapeutic Use (↑↓ Use): Depression
  • Action: Inhibition of neuronal uptake (Uptake, 70-80% NE removal) to enhance NE effect. High lipid solubility, cross BBB. CNS action. Have some M-receptor & α-receptor blocking activity. Important in cases of suicide attempt.
  • Adverse: Suicide risk, arrhythmia, myocardial ischemia, tachycardia, dry mouth, blurred vision, anxiety, agitation, panic attacks, insomnia
  • Notes: Also have sedative effect.
33
Q
  • *Tranylcypromine** (MAO- A, B; Parnate)
  • Pargyline* (MAO- B > A; Eutonyl)
  • Phenelzine* (MAO- A, B; Nardil)
  • Clorgiline* (MAO- A; Research Use)
  • *Selegiline** (MAO- B; Deprenyl)
A
  • Agent Type: Monoamine Oxidase (MAO) Inhibitors
  • Therapeutic Use (↑↓ Use): Depression (non-selective or MAOA inhibitors), Parkinson’s D. (MAOB inhibitors)
  • Action: Irreversible inhibition of MAO (2 isoforms: A & B). MAO more important than COMT.
  • Adverse: Suicide risk (for use in depression), tyramine effect (can cause HTN crisis, problem c non-selective or MAOA inhibitors, avoid tyramine-rich food (aged cheese, red wine, vegemite), anxiety, agitation, dizziness, arrhythmia, MI, hypotension.
  • Notes: Tyramine effect can lead to hypertensive crisis (action on gut MAO is important).
34
Q

Dopamine Antagonists (Antipsychotics)

  • *Haloperidol** (Aloperidin, Brotopon, Haldol, Halosten, Linton)
  • Chlorpromazine* (Thorazine, Largactil)
A
  • Agent Type: Dopamine Antagonists (Antipsychotics)
  • Therapeutic Use (↑↓ Use): Schizophrenia, severe anxiety, nausea, vomiting, aggressive episodes, vocal utterances of Tourette’s disorder.
  • Action: Dopamine-receptor blockers (chlorpromazine less potent than haloperidol). Typical antipsychotics. Use generally replaced by atypical antipsychotics (ie. Aripiprazole (Abilify), Olanzapine (Zyprexa) which have absence of extrapyramidal SE (↓prolactin elevation).
  • Adverse: Sedation, ↑ mortality in elderly c dementia-related psychosis, tachycardia, prolong QT interval, dyskinesis, ↑prolactin levels.
35
Q

Catechol-O-MethyTransferase (COMT) Inhibitors
[-capone]

  • *Tolcapone** (Tasmar)
  • *Entacapone** (Comtan)
A
  • Agent Type: Catechol-O-MethyTransferase (COMT) Inhibitors
  • Therapeutic Use (↑↓ Use): Parkinson’s Disease (usually reserved for last-line treatment)
  • Action: Reversible inhibition of COMT to prevent peripheral metabolism of L-dopa to allow ↑CNS access. COMT is less important than MAO. It is in tissues other than neurons (extraneuronal).
  • Adverse: Hepatoxicity, liver failure, dyskinesia,
    hypotension, nausea, dizziness, anxiety, sleep disorder
  • Notes: Unlike MAO inhibitors, it isn’t a concern c tyramine-rich food.
36
Q

Inamrinone

(Milrinone)

A
  • Agent Type: PDE Inhibitor
  • Therapeutic Use ( ↑↓ Use): Acute & Chronic HF
  • Action: Inhibit PDE III → ↑ cAMP→ ↑CO; Chronic (↑ mortality)
37
Q
  • Agent Type: Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Hypotension, shock (DOC, increasing in use), considered pressor agent (↑ BP).
  • Actions: Full agonist all receptors: α / β1 β2 β3 (weakest), neuronal, non-circulating, substrate for MAO & COMT. Does not cross BBB. Neuronal uptake inhibition →↑ effect (ie, c TCA, cocaine, atomoxetine).
  • CV:↑BP c reflex bradycardia. NE c atropine →↑BP c ↑HR
  • Notes: Short duration due to rapid metabolism. Given IV, IM, SC, not oral.
A

Norepinephrine

(Levarterenol)

38
Q
  • Agent Type: Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Anaphylaxis (DOC, allergic reactions), cardiogenic shock, cardiac arrest, glaucoma (↑outflow), severe bronchospasm. Not used for HF (↑O2 demand). Hypotension, ↑Shock, Pressor Agent
  • Actions: Full agonist all receptors: α / β1 β2 β3 (weakest), released from adrenal medulla, circulates, substrate for MAO & COMT. Does not cross BBB. Neuronal uptake inhibition →↑ effect (ie with TCA, cocaine).
  • Caution: Elderly, HTN, CV disease
  • CV: ↑ BP c ↑HR. EPI reversal (+α-blocker) →↓BP c ↑HR
  • Notes: Not oral.
A

Epinephrine

(generic)

39
Q
  • Agent Type: Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Shock syndrome (common use, ie. sepsis, Hi dose), acute HF (moderate dose). Can ↑ renal perfusion (D1-R).
  • Action: Full agonist all D-receptors, β1 (moderate dose), α1 (hi dose) , precursor to NE, substrate for MAO & COMT. NE/EPI precursor. Does not cross BBB.
  • Adverse: arrhythmias
  • Notes: Short duration. Not oral
A

Dopamine

(Intropin)

40
Q
  • Agent Type: Adrenoceptor Agonists- Dopamine
  • Therapeutic Use (↑↓ Use): Parkinson’s D, hyperprolactinemia (Bromo), restless leg S. (Prami).
  • Action: D-Agonists, Prami (some D3-sel)
  • Adverse: Hallucinations, drowsiness
A

Pramiprexole, Bromocriptine

41
Q
  • Agent Type: Adrenoceptor Agonists- Dopamine
  • Therapeutic Use (↑↓ Use): HTN crisis (Acute HTN), renal failure.
  • Action: Dopamine D1A-Receptor Agonist (activates AC, ↑cAMP)
  • Adverse: Tachycardia, ↑ocular pressure, can ↓serum K
  • Notes: Used short-term by IV infusion
A

Fenoldopam

(Corlopam)

42
Q
  • Agent Type: β-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Heart block (cardiac stimulant),asthma (rarely, many adverse effects)
  • Action: Full agonist all β receptors (activates AC, ↑cAMP), substrate for COMT but poor for MAO, doesn’t cross BBB.
  • Adverse: Tachycardia, palpitations, angina
  • CV: Decrease BP c tachycardia (direct & reflex).
  • Notes: synthetic- not endogenous. Longer duration than NE or EPI but still short duration.
A

Isoproterenol

(Isuprel)

43
Q
  • Agent Type: α1-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Nasal decongestant, hypotension considered pressor agent, glaucoma (↑outflow).
  • Action: Full agonist α1-receptors, little or no β-activity, activate PLC, ↑Ca ↑IP3.
  • Note: Not commonly used for hypotension
A

Phenylephrine

(Neosynephrine)

Methoxamine

(Vasoxyl)

44
Q
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Hypertension (CNS to
    ↓ sympathetic outflow), opioid withdrawal (↓severity)
  • Action: α2-agonists (inhibit AC, ↓cAMP), inhibits NE release, cross BBB.
  • Adverse: Dry mouth, sedation, impotence, rebound HTN, bradycardia.
  • Note: Need to discontinue gradually to prevent rebound HTN.
A

Clonidine

(Catapres)

Guanfacine

(Tenex)

45
Q
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Hypertension (CNS, ↓outflow)
  • Action: Prodrug → metabolizd to α-methyl-NE (α2-agonist (↓cAMP), inhibits NE release.
  • Note: Very good safety profile as anti-HTN during pregnancy
  • Adverse: Sedation, bradycardia , may cause positive
    direct Coombs test (RBC destruction), liver disease
A

α-Methyl Dopa

(Aldomet)

46
Q
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Premed surgical sedation
  • Action: Alpha2-agonist (inhibits AC, ↓cAMP), ↓NE release, crosses BBB.
  • Adverse: Hypotension, ↓HR (may cause sinus arrest)
  • Note: Little respiratory depression. ↑use
A

Dexmedetomidine

(Precedex)

47
Q
  • Agent Type: α2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Short-term muscle spasticity (ie. whiplash), multiple sclerosis
  • Action: Alpha2-agonist (inhibits AC, ↓cAMP), inhibits NE release, crosses BBB. CYP1A2 substrate
  • Adverse: Sedation, hypotension bradycardia, dry mouth.
A

Tizanidine

(Zanaflex)

48
Q
  • Agent Type: β-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Acute heart failure/ CHF (
  • Action: Profile of β1 agonist, Activate AC (↑cAMP), Substrate for COMT & MAO. Substrate for CYP3A4 metabolism.
  • Adverse: Arrhythmias, tolerance. don’t confuse c DA.
  • Notes: 4 isomers
A

Dobutamine

(Dobutrex)

49
Q
  • Agent Type: β2-Adrenoceptor Agonists
  • Therapeutic Use (↑↓ Use): Asthma, Bronchospasm (rescue inhaler), COPD, Premature labor (Ritodrine)
  • Action: β2-agonists, (activate AC, ↑cAMP), causes bronchodilation, relax uterus. Albuterol is short-acting but not substrate for COMT or MAO.
  • Action 2: Long-acting β2-agonists (LABAs) are available for chronic treatment ie. salmeterol, formoterol, arformoterol [-terol]. Have ↑risk respiratory death & severe attacks.
  • Adverse: Tachycardia, tremor, restlessness
  • Notes: Although Terbutaline is not FDA approved for premature labor, it is commonly used.
A

Albuterol (Proventil, Ventolin)

  • *Metaproterenol** (Alupent, Metaprel)
  • *Terbutaline** (Brethine, Brethaire)
  • *Ritodrine** (Yutopar)
  • *Salmeterol (LABA)** (Serevent, Diskus)
50
Q
  • Agent Type: Indirect Sympathomimetic Amine
  • Therapeutic Use (↑↓ Use): Nasal Decongestant, Red Eyes, orthostatic hypotension, appetite suppression
  • Action: Causes displacement of NE/DA & direct α- & β-receptor agonist. Can cross BBB to cause CNS
    stimulation. Enhanced effect c MAOI.
  • Adverse: Restlessness, tremor, insomnia, HTN, ↑HR
  • Notes: OTC
A

Ephedrine

(Vatronol, Efedron)

51
Q
  • Agent Type: Indirect Sympathomimetic Amine
  • Therapeutic Use (↑↓ Use): None, AA found in various foods (rich in aged cheese, red wine, liver, vegemite).
  • Action: Can cause a HTN crisis (↑BP, ↑HR) in pts receiving MAOI therapy (gut MAOA is important).
  • MAOs: Problem c non-selective MAO inhibitors (tranylcypromine) or MAOA selective (clorgyline) but not MAOB selective (selegiline) inhibitors.
  • Note: MAOA or non-selective MAO inhibitors used for
    depression treatment. MAOB selective inhibitors used for Parkinson’s D.
A

Tyramine (Amino-acid)

52
Q
  • Agent Type: Neurotransmitter Precursor
  • Therapeutic Use (↑↓ Use): Parkinson’s D. (assoc. c loss of dopaminergic fxn in midbrain, results in tremor, rigidity, bradykinesia & postural instability).
  • Action: L-dopa crosses BBB converted to dopamine.
  • Adverse: Dyskinesias (jerky, involuntary movement), vomiting & nausea (reduced c Carbidopa)
  • Notes: Given c Carbidopa (inhibits peripheral decarboxylation, doesn’t cross BBB). L-dopa effectiveness dec. after 4-5 yrs & a dopamine agonist (ie. pramiprexole) is added to pharmacotherapy regimen. Next is usually addition of a MAOB inhibitor..
A

L-Dopa/ Carbidopa

(Dopar, Larodopa)

53
Q
  • Agent Type: α-Adrenoreceptor Antagonist
  • Therapeutic Use (↑↓ Use): Acute & chronic
    pheochromocytoma, HTN crisis.
  • Action: Irreversible α-receptor antagonist (slight α1 over α2 selectivity, x5).
  • Adverse: Orthostatic (postural) hypotension, reflex ↑HR → arrhythmia, nasal congestion.
  • Both CV: ↓BP c reflex tachycardia. CV: EPI reversal (+α-blocker) → ↓BP c ↑HR
  • Notes: Can inhibit M-receptors, histamine, serotonin & neuronal uptake, Impotence
A

Phenoxybenzamine

(Dibenzyline)

54
Q
  • Agent Type: α-Adrenoreceptor Antagonist
  • Therapeutic Use (↑↓ Use): HT crisis, pheochromocytoma
  • Action: Non-selective, competitive α-receptor blocker. Block of pre-synaptic α2-receptors can ↑NE release.
  • Adverse: Orthostatic (postural) hypotension, reflex ↑HR → arrhythmia, nasal congestion.
  • Both CV: ↓BP c reflex tachycardia. CV: EPI reversal (+α-blocker) → ↓BP c ↑HR
  • Notes: low use
A

Phentolamine

(Tolazoline)

55
Q
  • Agent Type: α1-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): Benign prostatic hyperplasia (BPH), HTN, HTN crisis, Raynaud’s D.
  • Action: Selective, competitive α1-receptor blockers. Presynaptic α2-receptors unaffected → no reflex ↑HR (since α2-receptors operational). Tamsulosin α1A-selective.
  • Contra-indication: c PDE5 inhibitors ie Sildenafil (marked ↓BP)
  • Adverse: Orthostatic (postural) hypotension, nasal
    congestion.
  • Both CV: ↓BP s reflex tachycardia. EPI reversal (+α-blocker) → ↓BP c ↑HR
A

[-zosin]

  • *Prazosin** (Minipress)
  • *Terazosin** (Hytrin)
  • *Doxazosin** (Cardura)
  • *Tamsulosin (α1A-)** (Flomax)
56
Q
  • Agent Type: α2-Adrenoceptor Antagonists
  • Mirtazapine: competitive α2-receptor blocker. Used in depression treatment ie. PTSD. Can ↑appetite, ↑5-HT release (CNS). Adverse: sedation
  • Yohimbine: No FDA approved use. OTC for sexual
    dysfunction, impotence. In vet medicine, yohimbine is used to reverse xylazine action (α2- agonist, used in vet. medicine for anesthesia, analgesia, sedation)
  • Alkaloid, competitive α2-receptor blocker. May enhance effects of MAO inhibitors.
  • Adverse: HTN, tachycardia, insomnia, dizziness, anxiety, tremor
A

Mirtazapine (Mirtaz, Zispin)

Yohimbine (OTC)

57
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, angina, arrhythmias (SVT), HF (Metoplolol, Carvedilol), tremor, migraine, post-MI, mild hyperthyroidism (propranolol only), panic attack, stage fright (stress)
  • Action: β1 Selective (A-M), β Non-Selective (N-Z)
  • Adverse: Effects enhanced in elderly but clinical effectiveness is ↓ in elderly or Afro-Americans, fatigue, dizziness, ↓ myocardial reserve, cardiac depression, worsen asthma (block of bronchial β2-ARs, less c β1-ARs or those c ISA), peripheral vascular insufficiency (may precipitate/worsen Raynand’s D.), Diabetes (mask symptoms, hepatic β2 → ↓ recovery, less c β1-ARs or those c ISA), CNS (nightmares, mental depression, insomnia), withdrawal syndrome (supersensitivity, rebound HT, less with ISA).
A

β-Antagonists [-olol]

58
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, angina, arrhythmias (SVT), tremor, migraine, mild hyperthyroidism, panic attack, stage fright (stress), MI
  • Action: Non-Selective β-AR Antagonist, MSA (Membrane Stabilizing Activity) but NO Intrinsic Sympathomimetic Activity (ISA)
  • Adverse: See β-antagonist Slide
A

Propranolol

(Indreal)

59
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, Angina
  • Action: Non-Selective β-AR Antagonist, MSA (Membrane Stabilizing Activity), Intrinsic Sympathomimetic Activity (ISA)
  • Adverse: See β-antagonist Slide
A

Pindolol

(Visken)

60
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): Glaucoma (↓ Secretion), HTN, MI (Angina, Arrythmias)
  • Action: Non-Selective β-AR Antagonist, MSA (Membrane Stabilizing Activity), NO Intrinsic Sympathomimetic Activity (ISA), NO LA (Local Anaesthetic) Action.
  • Adverse: See β-antagonist Slide
A

Timolol

(Blocadren)

61
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, Angina, Arrythmias (SVT Common), MI, Heart Failure (HF)
  • Action: β1-Selective Antagonist, MSA (Membrane Stabilizing Activity), NO Intrinsic Sympathomimetic Activity (ISA), Local Anaesthetic Action.
  • Adverse: See β-antagonist Slide
A

Metoprolol

(Lopressor)

62
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN, Angina, Arrythmias, MI
  • Action: β1-Selective Antagonist, NO Intrinsic Sympathomimetic Activity (ISA), NO Local Anaesthetic Action.
  • Notes: Low Lipid Solubility (ie, CNS Action), Contraindication- Pregnant
  • Adverse: See β-antagonist Slide
A

Atenolol

(Tenormin)

63
Q
  • Agent Type: β-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): HTN (newest β-blocker)
  • Action: β1-Selective Antagonist (at doses NO Intrinsic Sympathomimetic Activity (ISA), NO Local Anaesthetic Action.
  • Notes: Low Lipid Solubility (ie, CNS Action)
  • Adverse: See β-antagonist Slide
A

Nebivolol

(Bystolic, Nebicip)

64
Q
  • Agent Type: β1-Adrenoceptor Antagonists
  • Therapeutic Use (↑↓ Use): Arrythmias, [angina]
  • Action: β1-Selective Antagonist, NO Intrinsic Sympathomimetic Activity (ISA), NO Local Anaesthetic Action.
  • Notes: Very short acting (10 min), used for arrythmias that arise during surgery.
  • Adverse: See β-antagonist Slide
A

Esmolol

(Brevablock)

65
Q
  • Agent Type: α/β-Adrenoceptor Antagonists
  • Carvedilol
    • Therapeutic Use (↑↓ Use): Heart failure (common), HTN
    • Action: α/β-Selective Antagonist, NO MSA (LA), NO Partial Agonist (ISA).
  • Labetalol
    • Therapeutic Use (↑↓ Use): Angina, HTN crisis, HTN
    • Action: α/β-Selective Antagonist, MSA (LA) & partial agonist activity (ISA).
  • Adverse: Bronchoconstriction, asthma, worsen diabetes, supersensitivity, insomnia, depression, ↓HR, ↓BP, sexual dysfunction, fasting hypoglycemia.
  • CV Acute: ↓BP & ↓ HR, ↓CO
A

Carvedilol (Coreg)

Labetalol (Normadyne)

66
Q
  • Agent Type: Indirect Sympathomimetics (Inhibit neuronal uptake)
  • Therapeutic Use (↑↓ Use): Local anesthetic, high drug abuse
  • Action: CNS stimulation, euphoria. LA-action (Na-channel block)
  • Adverse: HTN, myocardial ischemia, coronary spasm, arrhythmia
  • Notes: Inhibition of neuronal uptake (Uptake, 70-80% NE removal) to enhance NE effect. High lipid solubility.
  • Best Effect: Amphetamine Before Cocaine (ABC).
A

Cocaine

(generic)

67
Q
  • Agent Type: Indirect Sympathomimetics (Inhibit neuronal uptake)
  • Therapeutic Use (↑↓ Use): ADHD, considered as non-stimulant therapy
  • Action: Metabolized by CYP2D6.
  • Adverse: Arrhythmia, suicide tendency, myocardial
    ischemia, liver injury, agitation, panic attacks, insomnia.
  • Notes: Has less abuse potential than amphetamines (Ritalin, Methylphenidate).
A

Atomoxetine

(Strattera)

68
Q
  • Agent Type: Tricyclic antidepressants (TCAs)
    (Inhibit neuronal uptake)
  • Therapeutic Use (↑↓ Use): Depression
  • Action: Inhibition of neuronal uptake (Uptake, 70-80% NE removal) to enhance NE effect. High lipid solubility, cross BBB. CNS action. Have some M-receptor & α-receptor blocking activity. Important in cases of suicide attempt.
  • Adverse: Suicide risk, arrhythmia, myocardial ischemia, tachycardia, dry mouth, blurred vision, anxiety, agitation, panic attacks, insomnia
  • Notes: Also have sedative effect.
A
  • *Imipramine** (Tofrani)
  • *Amitriptyline** (Elavil)
69
Q
  • Agent Type: Monoamine Oxidase (MAO) Inhibitors
  • Therapeutic Use (↑↓ Use): Depression (non-selective or MAOA inhibitors), Parkinson’s D. (MAOB inhibitors)
  • Action: Irreversible inhibition of MAO (2 isoforms: A & B). MAO more important than COMT.
  • Adverse: Suicide risk (for use in depression), tyramine effect (can cause HTN crisis, problem c non-selective or MAOA inhibitors, avoid tyramine-rich food (aged cheese, red wine, vegemite), anxiety, agitation, dizziness, arrhythmia, MI, hypotension.
  • Notes: Tyramine effect can lead to hypertensive crisis (action on gut MAO is important).
A
  • *Tranylcypromine** (MAO- A, B; Parnate)
  • Pargyline* (MAO- B > A; Eutonyl)
  • Phenelzine* (MAO- A, B; Nardil)
  • Clorgiline* (MAO- A; Research Use)
  • *Selegiline** (MAO- B; Deprenyl)
70
Q
  • Agent Type: Dopamine Antagonists (Antipsychotics)
  • Therapeutic Use (↑↓ Use): Schizophrenia, severe anxiety, nausea, vomiting, aggressive episodes, vocal utterances of Tourette’s disorder.
  • Action: Dopamine-receptor blockers (chlorpromazine less potent than haloperidol). Typical antipsychotics. Use generally replaced by atypical antipsychotics (ie. Aripiprazole (Abilify), Olanzapine (Zyprexa) which have absence of extrapyramidal SE (↓prolactin elevation).
  • Adverse: Sedation, ↑ mortality in elderly c dementia-related psychosis, tachycardia, prolong QT interval, dyskinesis, ↑prolactin levels.
A

Dopamine Antagonists (Antipsychotics)

  • *Haloperidol** (Aloperidin, Brotopon, Haldol, Halosten, Linton)
  • Chlorpromazine* (Thorazine, Largactil)
71
Q
  • Agent Type: Catechol-O-MethyTransferase (COMT) Inhibitors
  • Therapeutic Use (↑↓ Use): Parkinson’s Disease (usually reserved for last-line treatment)
  • Action: Reversible inhibition of COMT to prevent peripheral metabolism of L-dopa to allow ↑CNS access. COMT is less important than MAO. It is in tissues other than neurons (extraneuronal).
  • Adverse: Hepatoxicity, liver failure, dyskinesia,
    hypotension, nausea, dizziness, anxiety, sleep disorder
  • Notes: Unlike MAO inhibitors, it isn’t a concern c tyramine-rich food.
A

Catechol-O-MethyTransferase (COMT) Inhibitors
[-capone]

  • *Tolcapone** (Tasmar)
  • *Entacapone** (Comtan)
72
Q
  • Agent Type: PDE Inhibitor
  • Therapeutic Use ( ↑↓ Use): Acute & Chronic HF
  • Action: Inhibit PDE III → ↑ cAMP→ ↑CO; Chronic (↑ mortality)
A

Inamrinone

(Milrinone)

PHARM (6 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions