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Flashcards in Last Minute Deck (22):
1

 

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

2

 

 

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.

3

 

 

 

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

4

 

 

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.

5

 

 

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

6

 

 

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

7

 


[-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

8

 

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

9

 

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

10

 

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

14

 

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.

15

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.

16

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.

17

 

 

Inamrinone

(Milrinone)

 

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

18

 

 

Bethanechol

(Urecholine)

  • Agent Type: M-receptor agonists: Limited clinical use, wide-action.
  • Therapeutic Use (↑↓ Use): Post-operative urinary retention, gut atony
  • Actions: M2, M3 > M1. Resistant to AchE. Doesn't cross BBB. Given SC or IM but not IV (Very Potent).
  • Adverse: SLUDGE; Sweating, salivation, lacrimation, urination, diarrhea, abdominal cramps, vomiting, hypotension, bradycardia, miosis, bronchospasm.

19

 

 

Pilocarpine (Ocusert-Pilo)

Carbachol (Carbacel)

Methacholine (Provocholine)

  • Agent Type: M-receptor agonists: Limited clinical use, wide-action.
  • Pilocarpine:
    • Therapeutic Use (↑↓ Use): DOC-Acute emergency glaucoma

    • Actions: Muscarinic activity; Resistant to AchE. Alkaloid, high lipid solubility, cross BBB. ↑outflow.

  • Carbachol: 
    • Therapeutic Use (↑↓ Use): Glaucoma, if pilocarpine ineffective

    • Actions: Muscarinic & some nicotinic activity; Resistant to AchE.

  • Methacholine
    • Therapeutic Use (↑↓ Use): Ocular procedures
    • Actions: Resistant to AchE. Does not cross BBB.
  • Other Therapeutic Use (↑↓ Use): dry mouth (xerostomia), bronchial challenge.
  • Adverse: SLUDGE; Sweating, salivation, lacrimation, urination, diarrhea, abdominal cramps, vomiting, hypotension, bradycardia, miosis, bronchospasm.

20

 

 

Organophosphate

Echothiophate  (Phospholine)

DFP (Isoflurophate)

Vx, Sarin, Soman (Nerve Gases)
 

  • Agent Type: Irreversible Cholinesterase Inhibitors, Organophosphates, OGs
  • Echothiophate & DFP
    • Therapeutic Use (↑↓ Use): Glaucoma (miosis, cycloplegia)
  • Nerve Gases
    • Use (↑↓ Use): Military, classified many 1000s

  • Actions: High lipid solubility, readily cross BBB, CNS actions.
  • Adverse: SLUDGE; Sweating, salivation, lacrimation,urination, diarrhea, abdominal cramps, vomiting, miosis, hypertension/hypotension, bradycardia, bronchospasm.
  • Toxicity treatment before aging: atropine + pralidoxime (2-PAM). AchE aging (DFP: 30-40 min, nerve g: sec/min)
  • Note: Muscle weakness (due to depolarizing block on N-receptors, this action is not reversible).

21

 

 

Scopolamine  (Isopto-Hyosine)

Propantheline   (Probanthine)

Glycopyrolate (Robinul, Glycate)
Pirenzepine (Gastrozepin)

  • Agent Type: Competitive, Muscarinic Receptor Antagonists
    • Scopolamine: 3-7 days action; Use: Motion sickness, diarrhea, ↓ Secretions
    • Propantheline: Probanthine, Quaternary Amine; Use: GI disorders ie, mild diarrhea, [peptic ulcer]
    • Glycopyrolate: GI disorders ie, mild diarrhea, [peptic ulcer]
    • Pirenzepine: Peptic Ulcer; M1 Selective
  • Adverse: ↓ Secretions, dry mouth, mydriasis, cycloplegia, constipation (↓ GI Activity), tachycardia, urine retention, hallucinations & excitation. Elderly more sensitive. Toxicity treatment c physostigmine (AchE inhibitor).
    • Hot as hell (thermoregulation). Blind as a bat (cycloplegia). Dry as a bone (↓ Secretions). Mad as a hatter (unresponsive, CNS delirium). Red as a beet (erythematous; direct vasodilation).

22

 

 

Benztropine

(Cogentin)

  • Agent Type: Competitive, Muscarinic Receptor Antagonists
  • Therapeutic Use (↑↓ Use): Parkinson's Disease, esp drug induced (improve tremor & rigidity but not bradykinesia)
  • Actions: Crosses BBB
  • Adverse: ↓ Secretions, dry mouth, mydriasis, cycloplegia, constipation (↓ GI Activity), tachycardia, urine retention, hallucinations & excitation. Elderly more sensitive. Toxicity treatment c physostigmine (AchE inhibitor).
    • Hot as hell (thermoregulation). Blind as a bat (cycloplegia). Dry as a bone (↓ Secretions). Mad as a hatter (unresponsive, CNS delirium). Red as a beet (erythematous; direct vasodilation).

23

 

 

Varenicline

(Chantix)

  • Agent Type: Nicotinic Receptor Agonist
  • Therapeutic Use (↑↓ Use): smoking cessation
  • Actions: Partial Agonist nicotinic receptors (ANS & NMJ).
    • Alkaloid, not endogenous, high lipid solubility. Readily crosses BBB. Widespread body action. Activates stimulatory & reward pathways. Prolonged stimulation (high toxic) causes depolarizing block similar to succinylcholine.
  • Adverse: ↑ Risk Depression, Suicide. Nausea
  • Acute CV: ↑BP, ↑HR, ↑respiration, ↓appetite

24

 

 

Mecamylamine

(Inversine)

  • Agent Type: Ganglionic Nicotinic Receptor (Non-Competetive) N-receptor Antagonists
  • Therapeutic Use (↑↓ Use): Resistant hypertension (drug of last resort)
  • Actions: Non-competitive, ganglionic N-receptor antagonist. Not frontline agent, drug of last resort. Good lipid solubility crosses BBB. Orally active.
  • Adverse: Widespread body action, many adverse side effects. Orthostatic (postural) hypotension, dizziness, ↓BP, ↑ HR, impotence, mydriasis, cycloplegia (blurred vision), constipation, urinary retention, muscle weakness, fatigue.
  • Note: Effective orally & has CNS action

25

 

 

Trimethaphan

(Arfonad)

  • Agent Type: Ganglionic Nicotinic Receptor (Competetive) N-receptor Antagonists
  • Therapeutic Use (↑↓ Use): Hypertensive Crisis (CNS origin), ↓ Blood Loss During Surgery
  • Actions: Competitive, Ganglionic N-receptor Antagonist. No CNS Action.
  • Adverse: Widespread body action, many adverse side effects. Orthostatic (postural) hypotension, dizziness, ↓ BP, ↑ HR, impotence, mydriasis, cycloplegia (blurred vision), constipation, urinary retention, muscle weakness, fatigue.
  • Note: Short Duration (10-15 min), inactive orally