ANS Sympathetic Drugs Flashcards by ايمان باني

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.

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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.

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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

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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

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Fenoldopam

(Corlopam)

Agent Type: Adrenoceptor Agonists- Dopamine
Therapeutic Use (↑↓ Use): HTN crisis (Acute HTN), renal failure.
Action: Dopamine D1_A-Receptor Agonist (activates AC, ↑cAMP)
Adverse: Tachycardia, ↑ocular pressure, can ↓serum K
Notes: Used short-term by IV infusion

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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.

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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

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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.

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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

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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

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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.

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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

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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.

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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

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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 MAO_A is important).
MAOs: Problem c non-selective MAO inhibitors (tranylcypromine) or MAO_A selective (clorgyline) but not MAO_B selective (selegiline) inhibitors.
Note: MAO_A or non-selective MAO inhibitors used for
depression treatment. MAO_B selective inhibitors used for Parkinson’s D.

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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..

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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

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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

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[-zosin]

*Prazosin** (Minipress)
*Terazosin** (Hytrin)
*Doxazosin** (Cardura)
*Tamsulosin (α_1A-)** (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 α_1A-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

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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

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β-Antagonists [-olol]

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).

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Propranolol

(Indreal)

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

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Pindolol

(Visken)

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

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Timolol

(Blocadren)

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

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**Metoprolol** (Lopressor)

* **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

**Atenolol** (Tenormin)

* **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

**Nebivolol** (Bystolic, Nebicip)

* **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

**Esmolol** (Brevablock)

* **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

**Carvedilol** (Coreg) **Labetalol** (Normadyne)

* **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

**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: A**mphetamine **B**efore **C**ocaine (ABC).

**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).

* *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.

* *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 MAO_A inhibitors), Parkinson’s D. (MAO_B 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 MAO_A 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).

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.

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.

**Inamrinone** (Milrinone)

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

* **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)

* **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)

* **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)

* **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***

* **Agent Type:** Adrenoceptor Agonists- Dopamine * **Therapeutic Use (↑↓ Use):** HTN crisis (Acute HTN), renal failure. * **Action:** Dopamine D1_A-Receptor Agonist (activates AC, ↑cAMP) * **Adverse:** Tachycardia, ↑ocular pressure, can ↓serum K * **Notes:** Used short-term by IV infusion

**Fenoldopam** (Corlopam)

* **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)

* **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)

* **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)

* **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)

* **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)

* **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)

* **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)

* **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)

* **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)

* **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 MAO_A is important). * **MAOs:** Problem c non-selective MAO inhibitors (tranylcypromine) or MAO_A selective (clorgyline) but not MAO_B selective (selegiline) inhibitors. * **Note:** MAO_A or non-selective MAO inhibitors used for depression treatment. MAO_B selective inhibitors used for Parkinson’s D.

**Tyramine** (Amino-acid)

* **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)

* **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)

* **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)

* **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 α_1A-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 (α_1A-)** (Flomax)

* **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)

* **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]**

* **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)

* **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)

* **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)

**Metoprolol** (Lopressor)

**Atenolol** (Tenormin)

**Nebivolol** (Bystolic, Nebicip)

**Esmolol** (Brevablock)

**Carvedilol** (Coreg) **Labetalol** (Normadyne)

**Cocaine** (generic)

**Atomoxetine** (Strattera)

* *Imipramine** (Tofrani) * *Amitriptyline** (Elavil)

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

Dopamine Antagonists (Antipsychotics) * *Haloperidol** (Aloperidin, Brotopon, Haldol, Halosten, Linton) * **Chlorpromazine*** (Thorazine, Largactil)

Catechol-O-MethyTransferase (COMT) Inhibitors [-capone] * *Tolcapone** (Tasmar) * *Entacapone** (Comtan)

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

**Inamrinone** (Milrinone)