ANS Treatment + Flashcards
Treatment:
Bradycardia
or Heart Block
Due to Excess Vagal Tone
Atropine
Natural, Tertiary Alkaloid, Lipid-Soluble, CNS; Competitive Antagonist, Muscarinic Blocker
Treatment:
Emergency
Cardiac Arrest
or Heart Block
Epinephrine
Agonist @ Alpha, Beta 1, Beta 2
Treatment:
Arrhythmia
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Angina
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Post-MI
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Acute Unstable CHF
Dobutamine
(Beta 1 Agonist, Direct-Acting; Acts @ Beta 1 and Alpha 1)
_Beta 1: Stimulate Heart
_Alpha 1: Vasoconstriction
⇒ Raise Blood Pressure
Treatment:
Chronic, Stable CHF
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Cardiac Manifestations of Hyperthyroidism
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Local Anesthesic Preps (for Vasoconstriction):
Epinphrine
Agonist @ Alpha, Beta 1, Beta 2
Treatment:
Anaphylactic Shock (IV) (Acute Hypersensitivity Reaction)
Epinephrine (Drug of Choice):
(Agonist @ Alpha, Beta 1, Beta 2)
_Alpha 1: Vasoconstriction
⇒ Raise Blood Pressure
_Beta 1: Stimulate Heart
_Beta 2: Bronchodilation
Treatment:
Shock
Dopamine
(Agonist @ Alpha 1, Beta 1, DA)
(Precursor of NE and Epi)
_Alpha 1: Vasoconstriction
⇒ Raise Blood Pressure
_Beta1: Stimulate Heart
_D1 Receptor: Renal Artery Dilation
(Protects Kidney, whereas NE vasoconstricts Renal)
Treatment:
Hypotension
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
Treatment:
Hypertension
(First-Line: Uncomplicated, Essential Chronic HTN; Less effective in Black Patients)
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
______________________
1) Clonidine
(Alpha 2 Agonist, Direct-Acting)
(@ Brainstem Medulla to Inhibit Sympathetic)
2) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
(@ CNS to Inhibit Sympathetic)
3) Tizanidine
(Alpha 2 Agonist, Direct-Acting)
______________________
1) Prazosin
(Selective Alpha 1 Antagonist)
(Chronic HTN: oral; Emergency: Inj.)
2) Tamsulosin
(Selective Alpha 1 Antagonist)
3) Labetalol
(Competitive Block @ both Alpha 1 and Beta)
4) Carvedilol
(Competitive Block @ both Alpha 1 and Beta)
______________________
Reserpine:
(Inhibits intra-neuronal storage of NE: Inhibits Transport of NE from Cytosol to Vesicle)
_(Leads to Gradual Depletion of NE and 5-HT Stores) (Little use now)
_(Adverse Effects: Lethargy, Diarrhea, Depression-very long lasting)
Treatment:
COPD
1) Ipratropium
(Via BronchoDilation )
(Quaternary, Ionized;
Competitive Antagonist, Muscarinic Blocker)
2) Tiotropium
(Via BronchoDilation )
(Quaternary, Ionized;
Competitive Antagonist, Muscarinic Blocker)
Treatment:
Asthma
1) Epinphrine (Via Bronchodilation )
(Severe Asthma)
(Agonist @ Alpha, Beta 1, Beta 2)
2) Albuterol
(Beta 2 Agonist, Direct-Acting)
(Via Bronchodilation)
3) Salmeterol
(Beta 2 Agonist, Direct-Acting)
(Via Bronchodilation)
4) Ritodrine
(Beta 2 Agonist, Direct-Acting)
(Via Bronchodilation)
Treatment:
Constipation (lack of tone)
Bethanechol
(Direct-Acting, Agonist,
Selective on smooth muscle @ GI, @ Bladder)
Treatment:
Post-Operative Ileus (Atony)
Neostigmine (Quaternary, Ionized; Indirect-Acting, Reversible Anti-Cholinesterase, False Substrate)
Treatment:
Diarrhea
Atropine (Lomotil)
(Source of atropine poisoning in children)
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
Treatment:
Motion Sickness (Emesis)
Scopolamine (Natural, Tertiary Alkaloid, Lipid-Soluble, CNS; Competitive Antagonist, Muscarinic Blocker)
Treatment:
Bowel Spasms
Irritable Bowel Syndrome, IBS
Dicyclomine (Synthetic, Tertiary, Lipid-Soluble, CNS; Competitive Antagnoist, Muscarinic Blocker)
Treatment:
Urinary Retention
Bethanechol
(Direct-Acting, Agonist,
Selective on smooth muscle @ GI, @ Bladder)
Treatment:
Benign Prostatic Hypertrophy (BPH): Relax Urethral Smooth Muscle; Promotes Urine Flow
1) Prazosin
(Selective Alpha 1 Antagonist)
(Chronic HTN: oral; Emergency: Inj.)
2) Tamsulosin*
(Selective Alpha 1 Antagonist)
3) Labetalol
(Competitive Block @ both Alpha 1 and Beta)
4) Carvedilol
(Competitive Block @ both Alpha 1 and Beta)
Treatment:
Urinary Frequency/Urgency, Overactive Bladder
1) Oxybutynin
(Quaternary; Some M3 Selectivity, Muscarinic Blocker)
2) Solifenacin
(Quaternary; Better M3 Selectivity, Muscarinic Blocker)
3) Tolteridine
(Quaternary; M3 Selective,
Muscarinic Blocker)
4) Mirabegron
(Beta 3 Agonist, Direct-Acting;
Beta 3 Relaxes Bladder Smooth Muscle)
Treatment:
Premature Labor
1) Albuterol
(Beta 2 Agonist, Direct-Acting)
(Uterine Relaxation @ Beta 2)
2) Salmeterol
(Beta 2 Agonist, Direct-Acting)
(Uterine Relaxation @ Beta 2)
3) Ritodrine*
(Beta 2 Agonist, Direct-Acting)
(Uterine Relaxation @ Beta 2)
Treatment:
Xerostomia
Pilocarpine
(Direct-Acting, Agonist,
Muscarinic, Tertiary Alkaloid, Lipid-Soluble, CNS)
Treatment:
Excess Salivation (Hyperhidrosis)
1) Atropine
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist, Muscarinic Blocker)
2) Botulinum Toxin
(Inhibits ACh Release)
Treatment:
Nasal Congestion
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
Treatment:
Glaucoma
1) Clonidine
(Alpha 2 Agonist, Direct-Acting;
Reduces Aqueous Humor Formation)
2) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
3) Tizanidine
(Alpha 2 Agonist, Direct-Acting)
_____________________
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol*
(Non-Selective Beta Antagonist)
(Reduces Aqueous Humor Formation)
5) Pindolol
(Non-Selective Beta Partial Agonist)
__________________
Pilocarpine
(Direct-Acting, Agonist,
Muscarinic, Tertiary Alkaloid,
Lipid-Soluble, CNS)
Ophthalmologic Exam:
Trigger Mydriasis (Dilated Pupils)
and
Cycloplegia (Ciliary Muscle Paralysis):
Tropicamide
(Synthetic, Tertiary, Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
Treatment:
Migraine Prophylaxis
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Migraines
Botulinum Toxin
Inhibits ACh Release
Treatment:
Wrinkles
Botulinum Toxin
Inhibits ACh Release
Treatment:
Local Muscle Spasms
Botulinum Toxin (Inhibits ACh Rlease)
Treatment:
Spasticity due to Neuropathy (e.g. Cerebral Palsy):
1) Clonidine*
(Alpha 2 Agonist, Direct-Acting)
(@ Spinal Cord to Reduce firing to motor neurons)
2) Tizanidine*
(Alpha 2 Agonist, Direct-Acting)
(@ Spinal Cord)
3) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
Treatment:
Tremor (of Peripheral origin)
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Treatment:
Alzheimer’s
1) Donepezil
(Centrally-Acting
Reversible Anti-Cholinesterase;
Lipid-Soluble, CNS)
2) Rivastigmine
(Centrally-Acting
Reversible Anti-Cholinesterase;
Lipid-Soluble, CNS)
3) Galantamine
(Centrally-Acting
Reversible Anti-Cholinesterase;
Lipid-Soluble, CNS)
4) Tacrine
(Centrally-Acting
Reversible Anti-Cholinesterase;
Lipid-Soluble, CNS)
Treatment:
Parkinson’s
1) Benztropin
(Synthetic, Tertiary, Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
2) Trihexyphenidyl
(Synthetic, Tertiary, Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
3) Selegiline
(MAO-B Inhibitor; Indirect-Acting;
Inhibits Dopamine Metabolism @ Brain)
4) COMT Inhibitors
(Indirect-Acting;
Inhibit Dopamine Metabolism @ Brain)
Treatment:
ADHD
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis) \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
1) Clonidine
(Alpha 2 Agonist, Direct-Acting)
(Not First-line; Not as effective as Central Stimulants)
2) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
3) Tizanidine
(Alpha 2 Agonist, Direct-Acting)
Treatment:
Narcolepsy
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
Treatment:
Depression
1) Tricyclic Antidepressants
(Indirect-Acting;
Inhibit NE Reuptake)
2) MAO-A Inhibitors
(Indirect-Acting;
Inhibits NT Metabolism)
Treatment:
Pain Syndromes
1) Tricyclic Antidepressants
(Indirect-Acting;
Inhibit NE Reuptake)
2) Cocaine (Indirect-Acting; Inhibit NE Reuptake and Inhibit Dopamine Reuptake) (Not Rx)
Treatment:
Antimuscarinic Poisoning
e.g. Atropine Poisoning
1) Physostigmine (Tertiary, Lipid-Soluble, CNS; Indirect-Acting, Reversible Anti-Cholinesterase, False Substrate)
2) Neostigmine (Quaternary, Ionized; Indirect-Acting, Reversible Anti-Cholinesterase, False Substrate)
Treatment:
Organophosphate Poisoning:
1) Pralidoxime
(Oxime; within 1 hour of poisoning, before Aging!)
2) (NO!!) Pyridostigmine
(Reversible Anti-cholinesterase;
Prophylaxis: Gulf War Syndrome with repeated use)
(Gulf War Syndrome: Muscle Aches and Weakness, Diarrhea, Fatigue, Cognitive Problems)
Reversal of Competitive Muscle Blockers
Atropine + Reversible Anti-Cholinesterase
Atropine (Natural, Tertiary Alkaloid, Lipid-Soluble, CNS; Competitive Antagonist, Muscarinic Blocker)
Diagnostic:
Myasthenia Gravis
Edrophonium (Truly Reversible, Competitive, Short-Acting; Indirect-Acting Anti-Cholinesterase)
Diagnostic:
Asthma: Inhalation Challenge (Hyper Bronchoconstriction):
Metacholine
(Direct-Acting, Agonist, Muscarinic,
Affinity @ Heart;
Inhalation Challenge: Bronchoconstriction)
Adverse Effects:
Cholinergic Poison:
1) Echothiophate
(Irreversible Anti-Cholinesterase,
Organophosphate;
Long-Acting Miotic)
2) Malathion
(Irreversible Anti-Cholinesterase,
Organophosphate; Insecticide)
3) Sarin
(Irreversible Anti-Cholinesterase;
Nerve Gas)
Adverse Effects:
Anti-Muscarinic Poison:
Atropine (Natural, Tertiary Alkaloid, Lipid-Soluble, CNS; Competitive Antagonist, Muscarinic Blocker)
@ Low Therapeutic Doses: No Detectable CNS Effects @ Toxic Doses: CNS Stimulation, Restlessness, Irritability, Disorientation, Hallucinations.
@ Small Doses: 1) Hot, Flushed, Dry Skin, 2) Decreased Sweating (M3 Block), 3) Dry Mouth, Decreased Salivation (M3 Block), Thirst
@ Larger Doses: 1) Dilated Pupils (Photophobia) (Mydriasis) (M3 Circular Muscle Paralysis),
2) Blurry Near Vision (Cycloplegia) (M3 Ciliary Muscle Paralysis),
3) Tachycardia (Palpitations) (M2 Vagal Block)
@ Even Larger Doses: Anti-Muscarinic Effects
Red as a Beet, Hot as a Hare, Dry as a Bone, Blind as a Bat, Mad as a Hatter
______________________
Scopolamine
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
1) CNS Depressant:
Drowsiness, Amnesia:
Scopolamine @ Clinical Doses
2) CNS Excitation: Hallucinations:
Scopolamine @ Patients
w/ Severe Pain!
Adverse Effects:
Cardiac Stimulation
1) @ Beta 1: Albuterol
(Beta 2 Agonist, Direct-Acting)
2) @ Beta 1: Salmeterol
(Beta 2 Agonist, Direct-Acting)
3) @ Beta 1: Ritodrine
(Beta 2 Agonist, Direct-Acting)
4) @ Beta 1: Mirabegron
(Beta 3 Agonist, Direct-Acting;
Beta 3 Relaxes Bladder Smooth Muscle)
Adverse Effects:
Arrhythmias
1) Metacholine
(Direct-Acting, Agonist, Muscarinic,
Affinity @ Heart;
Inhalation Challenge: Bronchoconstriction)
2) @ Beta 1: Dobutamine
(Beta 1 Agonist, Direct-Acting;
Acts @ Beta 1 and Alpha 1)
Adverse Effects:
Heart Block
Metacholine
(Direct-Acting, Agonist, Muscarinic,
Affinity @ Heart;
Inhalation Challenge: Bronchoconstriction)
Adverse Effects:
Hyperkalemia ⇒ Cardiac Depression
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
(More common in Burn, Trauma pts; Dangerous if on Digoxin)
Adverse Effects:
Bradycardia
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
(Via Muscarinic Stimulation)
_______________________
@ Alpha 1:
Hypertension + Reflex Bradycardia:
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
Adverse Effects:
Tachycardia
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
Adverse Effects:
Reflex Tachycardia
1) Prazosin
(Selective Alpha 1 Antagonist)
(Chronic HTN: oral; Emergency: Inj.)
2) Tamsulosin
(Selective Alpha 1 Antagonist)
3) Labetalol
(Competitive Block @ both Alpha 1 and Beta)
4) Carvedilol
(Competitive Block @ both Alpha 1 and Beta)
Adverse Effects:
Hypotension
1) Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
(Via Histamine Release andGanglionic Block)
2) d-Tubocurarine (Quaternary Alkaloid; Non-Depolarizing = Competitive Antagonist @ NMJ, Nicotinic)
(Via Histamine Release)
Adverse Effects:
Postural Hypotension
(very Marked)
Due to Blockage of Reflex Vasoconstriction
1) Prazosin
(Selective Alpha 1 Antagonist)
(Chronic HTN: oral; Emergency: Inj.)
2) Tamsulosin
(Selective Alpha 1 Antagonist)
3) Labetalol
(Competitive Block @ both Alpha 1 and Beta)
4) Carvedilol
(Competitive Block @ both Alpha 1 and Beta)
Adverse Effects:
Hypertension
@ Alpha 1: Dobutamine
(Beta 1 Agonist, Direct-Acting;
Acts @ Beta 1 and Alpha 1)
______________________
@ Alpha 1: + Reflex Bradycardia:
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
@ Alpha 1: + Reflex Bradycardia:
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
@ Alpha 1: + Reflex Bradycardia:
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
______________________
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
Adverse Effects:
Rebound Hypertension
1) Clonidine
(Alpha 2 Agonist, Direct-Acting)
(@ Brainstem Medulla to Inhibit Sympathetic)
2) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
(@ CNS to Inhibit Sympathetic)
3) Tizanidine
(Alpha 2 Agonist, Direct-Acting)
Adverse Effects:
Increased Bronchial Secretions
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
(Via Muscarinic Stimulation)
Adverse Effects:
Bronchoconstriction
(Via Beta 2 Block)
Asthma Pts
⇒ Use Selective Beta 1 Blockers
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Adverse Effects:
Fasciculations of Abdominal Muscles ⇒ Increases Intragastric Pressure ⇒ Risk of Reflux
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
(Most likely in pts w/ Delayed Gastric Emptying: Diabetics, Morbid Obesity)
Adverse Effects:
Urinary Retention
Atropine (Natural, Tertiary Alkaloid, Lipid-Soluble, CNS; Competitive Antagonist, Muscarinic Blocker) \_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_\_
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
(@ Urinary Sphincter;
esp. Old Men, Enlarged Prostate)
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
(@ Urinary Sphincter;
esp. Old Men, Enlarged Prostate)
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
(@ Urinary Sphincter;
esp Old Men, Enlarged Prostate)
Adverse Effects:
Increased Intraocular Pressure
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
Adverse Effects:
Malignant Hyperthermia
⇒ Treat this with Dantrolene
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
Adverse Effects:
Post-Operative Muscle Pain
Succinylcholine
(Depolarizing = Partial Agonist
@ NMJ, Nicotinic;
Plasma Pseudocholinesterase)
Adverse Effects:
Tremors
@ Beta 2 @ Skeletal Muscle:
1) Albuterol
(Beta 2 Agonist, Direct-Acting)
2) Salmeterol
(Beta 2 Agonist, Direct-Acting)
3) Ritodrine
(Beta 2 Agonist, Direct-Acting)
______________________
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
Adverse Effects:
Muscle Weakness
1) Clonidine
(Alpha 2 Agonist, Direct-Acting)
(@ Brainstem Medulla to Inhibit Sympathetic)
2) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
(@ CNS to Inhibit Sympathetic)
3) Tizanidine
(Alpha 2 Agonist, Direct-Acting)
Adverse Effects:
Rebound Nasal Congestion: (Rhinitis Medicamentosa)
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
Adverse Effects:
Hypoglycemia
Via Beta 1 Block @ Liver
of Compensatory Hyperglycemic Effects of Epinephrine
Sweating is Only Remaining Symptom!
(Loss of Tremor, Palpitations)
Diabtic Pts ⇒ Use Selective Beta 1 Blockers
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Adverse Effects:
CNS Depressant: Drowsiness, Amnesia
Scopolamine @ Clinical Doses
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
Adverse Effects:
Sedation
1) Clonidine
(Alpha 2 Agonist, Direct-Acting)
(@ Brainstem Medulla to Inhibit Sympathetic)
2) Alpha-Methyldopa
(Alpha 2 Agonist, Direct-Acting)
(@ CNS to Inhibit Sympathetic)
3) Tizanidine
(Alpha 2 Agonist, Direct-Acting)
Adverse Effects:
Nightmares/Sleep Disturbances
Propranolol has High Lipid Solubility.
Atenolol is Less Lipid Soluble
1) Propranolol
(Non-Selective Beta Antagonist; High Lipid Solubility)
2) Metoprolol
(Selective Beta 1 Antagonist)
3) Atenolol
(Selective Beta 1 Antagonist)
4) Timolol
(Non-Selective Beta Antagonist)
5) Pindolol
(Non-Selective Beta Partial Agonist)
Adverse Effects:
CNS Stimulation: e.g. Insomnia
1) Phenylephrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
2) Oxymetazoline
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
3) Pseudoephedrine
(Alpha 1 Agonist, Direct-Acting)
(Vasoconstriction)
Adverse Effects:
CNS Excitation: Hallucinations
Scopolamine
@ Patients w/ Severe Pain!
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
Adverse Effects:
CNS Excitation: Restlessness, Irritability, Disorientation, Hallucinations
Atropine @ Toxic Doses
(No CNS @ Therapeutic Doses)
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
Adverse Effects:
Psychosis, Convulsions, Dependence
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
Contraindications:
Atropine
(Natural, Tertiary Alkaloid,
Lipid-Soluble, CNS;
Competitive Antagonist,
Muscarinic Blocker)
1) Narrow Angle Glaucoma
(Atropine causes Ciliary muscle to block flow)
2) Prostatic Hypertrophy
(Old Men)
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Beta Blockers: Propranolol, Atenolol, Metoprolol, Pindolol, Timolol
1) Unstable/Decompensated CHF
2) Acute CHF
3) Diabetic Pts:
Use Selective Beta 1 Blockers
4) Asthma Pts:
Use Selective Beta 1 Blockers
Drug Interactions:
Diazepam
1) Increases Duration of Non-Depolarizing Blockers
(Competitive Antagonists)
2) Decreases Duration of Depolarizing Blockers
(Partial Agonists) (Succinylcholine)
Drug Interactions:
Aminoglycosides
Increase Intensity and Duration of Muscle Blockers
(Both Non-Depolarizers and Depolarizers)
Large Doses can cause Muscle Block on its own
Drug Interactions:
Ester Local Anesthetics
Increase Duration of Succinylcholine
b/c also Broken Down by Pseudocholinesterase
Drug Interactions:
Cholinesterase Inhibitors
Neostigmine, Organophosphate Insecticides, etc.
Increase Duration of Succinylcholine
Drug Interactions:
MAO Inhibitors
⇒ Hypertensive Crisis
1) Amphetamine (Indirect-Acting; Stimulates NE Release; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
2) Methamphetamine (Indirect-Acting; Stimulates NE Release; Greater CNS Activity than Amphetamine) (Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
3) Ephedrine (Mixed Action: Direct @ Alpha, Beta; and Indirect @ Stimulates RE Release) (Milder than Amphetamines; Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
4) Tyramine: @ Food
(Indirect-Acting;
Stimulates NE Release)
(Tachyphylaxis; MAOI Intrxn: Hypertensive Crisis)
