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Flashcards in ANS Sympathetic Drugs Deck (72):
1

 

 

 

Norepinephrine

(Levarterenol)

  • 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.

2

 

 

 

Epinephrine

(generic)

  • 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.

3

 

 

 

Dopamine

(Intropin)

  • 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

4

 

 

 

Pramiprexole, Bromocriptine

  • 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

5

 

 

 

Fenoldopam

(Corlopam)

  • 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

6

 

 

 

Isoproterenol

(Isuprel)

  • 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.

7

 

Phenylephrine

(Neosynephrine)

 

Methoxamine

(Vasoxyl)

  • 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

8

 

 

Clonidine

(Catapres)

Guanfacine

(Tenex)

  • 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.

9

 

 

α-Methyl Dopa

(Aldomet)

  • 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

10

 

 

Dexmedetomidine

(Precedex)

  • 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

11

 

 

Tizanidine

(Zanaflex)

  • 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.

12

 

 

 

Dobutamine

(Dobutrex)

  • 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

13

 

 

Albuterol (Proventil, Ventolin)

Metaproterenol (Alupent, Metaprel)
Terbutaline (Brethine, Brethaire)
Ritodrine (Yutopar)
Salmeterol (LABA) (Serevent, Diskus)

  • 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.

14

 

 

 

Ephedrine

(Vatronol, Efedron)

  • 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

15

 

 

 

Tyramine (Amino-acid)

 

  • 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.

16

 

 

 

L-Dopa/ Carbidopa

(Dopar, Larodopa)

 

  • 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..

17

 

 

 

Phenoxybenzamine

(Dibenzyline)

  • 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

18

 

 

 

Phentolamine

(Tolazoline)

  • 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

19

 


[-zosin]

Prazosin (Minipress)
Terazosin (Hytrin)
Doxazosin (Cardura)
Tamsulosin (α1A-) (Flomax)

  • 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

20

 

Mirtazapine (Mirtaz, Zispin)
 

Yohimbine (OTC)

  • 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

21

 

β-Antagonists [-olol]

 

Q image thumb

 

  • 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).

22

 

Propranolol

(Indreal)

 

Q image thumb

  • 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

23

 

Pindolol

(Visken)

 

Q image thumb

  • 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

24

 

Timolol

(Blocadren)

 

Q image thumb

  • 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

25

 

Metoprolol

(Lopressor)

 

Q image thumb

  • 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

26

 

Atenolol

(Tenormin)

 

Q image thumb

  • 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

27

 

Nebivolol

(Bystolic, Nebicip)

 

Q image thumb

  • 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

28

 

Esmolol

(Brevablock)

 

Q image thumb

  • 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

29

 

Carvedilol (Coreg)

Labetalol (Normadyne)

 

Q image thumb

  • 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

 

Cocaine

(generic)

 

  • 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

 

Atomoxetine

(Strattera)

 

  • 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

 

Imipramine (Tofrani)
Amitriptyline (Elavil)

 

  • 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

 

Tranylcypromine (MAO- A, B; Parnate)
Pargyline (MAO- B > A; Eutonyl)
Phenelzine (MAO- A, B; Nardil)
Clorgiline (MAO- A; Research Use)
Selegiline (MAO- B; Deprenyl)

 

  • 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

Dopamine Antagonists (Antipsychotics)

 

Haloperidol (Aloperidin, Brotopon, Haldol, Halosten, Linton)
Chlorpromazine (Thorazine, Largactil)

 

  • 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

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

 

Tolcapone (Tasmar)
Entacapone (Comtan)

 

  • 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

 

 

Inamrinone

(Milrinone)

 

  • Agent Type: PDE Inhibitor
  • Therapeutic Use ( ↓ Use): Acute & Chronic HF
  • Action: Inhibit PDE III → ↑ cAMP→ ↑CO; Chronic (↑ mortality)

37

  • 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.

 

 

 

Norepinephrine

(Levarterenol)

38

  • 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.

 

 

 

Epinephrine

(generic)

39

  • 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

 

 

 

Dopamine

(Intropin)

40

  • 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

 

 

 

Pramiprexole, Bromocriptine

41

  • 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

 

 

 

Fenoldopam

(Corlopam)

42

  • 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.

 

 

 

Isoproterenol

(Isuprel)

43

  • 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

 

Phenylephrine

(Neosynephrine)

 

Methoxamine

(Vasoxyl)

44

  • 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.

 

 

Clonidine

(Catapres)

Guanfacine

(Tenex)

45

  • 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

 

 

α-Methyl Dopa

(Aldomet)

46

  • 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

 

 

Dexmedetomidine

(Precedex)

47

  • 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.

 

 

Tizanidine

(Zanaflex)

48

  • 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

 

 

 

Dobutamine

(Dobutrex)

49

  • 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.

 

 

Albuterol (Proventil, Ventolin)

Metaproterenol (Alupent, Metaprel)
Terbutaline (Brethine, Brethaire)
Ritodrine (Yutopar)
Salmeterol (LABA) (Serevent, Diskus)

50

  • 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

 

 

 

Ephedrine

(Vatronol, Efedron)

51

  • 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.

 

 

 

Tyramine (Amino-acid)

 

52

  • 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..

 

 

 

L-Dopa/ Carbidopa

(Dopar, Larodopa)

 

53

  • 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

 

 

 

Phenoxybenzamine

(Dibenzyline)

54

  • 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

 

 

 

Phentolamine

(Tolazoline)

55

  • 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

 


[-zosin]

Prazosin (Minipress)
Terazosin (Hytrin)
Doxazosin (Cardura)
Tamsulosin (α1A-) (Flomax)

56

  • 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

 

Mirtazapine (Mirtaz, Zispin)
 

Yohimbine (OTC)

57

 

  • 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).

 

β-Antagonists [-olol]

 

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58

  • 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

 

Propranolol

(Indreal)

 

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59

  • 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

 

Pindolol

(Visken)

 

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60

  • 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

 

Timolol

(Blocadren)

 

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61

  • 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

 

Metoprolol

(Lopressor)

 

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62

  • 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

 

Atenolol

(Tenormin)

 

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63

  • 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

 

Nebivolol

(Bystolic, Nebicip)

 

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64

  • 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

 

Esmolol

(Brevablock)

 

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65

  • 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

 

Carvedilol (Coreg)

Labetalol (Normadyne)

 

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66

  • 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).

 

Cocaine

(generic)

 

67

  • 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).

 

Atomoxetine

(Strattera)

 

68

  • 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.

 

Imipramine (Tofrani)
Amitriptyline (Elavil)

 

69

  • 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).

 

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

  • 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.

Dopamine Antagonists (Antipsychotics)

 

Haloperidol (Aloperidin, Brotopon, Haldol, Halosten, Linton)
Chlorpromazine (Thorazine, Largactil)

 

71

  • 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.

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

 

Tolcapone (Tasmar)
Entacapone (Comtan)

 

72

  • Agent Type: PDE Inhibitor
  • Therapeutic Use ( ↓ Use): Acute & Chronic HF
  • Action: Inhibit PDE III → ↑ cAMP→ ↑CO; Chronic (↑ mortality)

 

 

Inamrinone

(Milrinone)