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Test 1, autonomics etc
General principles, autonomics, antiepilectic, basal ganglia
99
Pharmacology
Graduate
01/12/2012

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Term
Acetylcysteine
Definition
Used to replace hepatic cysteine in acetaminophen OD (Lecture 2)
Term
Acetaminophen
Definition
Analgesic, antipyretic, metabolized by liver
Term
Phenobarbital
Definition
Barbiturate, sedative/hypnotic. Important now bc at pH 6 - poor renal excretion. At pH 8, excretion increased (Lecture 2)
Term
Reserpine
Definition
Blocks dopamine transport into vesicle at noradrenergic synapse (Lecture 5)
Term
Guanethidine
Definition
Block release of NE, ATP, DBH. Initial ^BP, then long-term decrease (indirect sympathomimetic) (Lecture 5)
Term
Cocaine
Definition
Block reuptake of NE, 5HT, DA into varicosity (Lecture 5)
Term
Alpha-methyl-dopa
Definition
Similar to DOPA, acts on CNS to decrease SNS outflow. Becomes alpha-methyl-NE which stimulates inhibitory areas in the medulla -> decreased BP
Term
Tyramine
Definition
Converts to octopamine (false transmitter). Releases nonvesicular NE - indirectly acting adrenergic agonist. Wine and cheese syndrome (Lecture 6)
Term
Epinephrine
Definition
Alpha, Beta-1, Beta-2 agonist. Best stimulator of Alpha (vasoconstriction -> ^TPR -> ^BP). Used for hypersensitivity, cardiac arrest, adjuncts to local anesth
Term
Norepinephrine
Definition
Stimulates only Beta-1 and Alpha. Alpha dominates so NE administration causes ^TPR with decreased HR (vagal dominance). Used for shock (not often)
Term
Dopamine
Definition
Renal vasodilation at low [], Beta-1 at higher, Alpha at even higher. Used to treat shock by increasing dose to stimulate appropriate receptors.
Term
Isoproterenol
Definition
Only Beta-1 and Beta-2 receptors stimulated. Stimulates Beta best of Iso/NE/Epi. Not useful, but may be used for asthma
Term
Phenylephrine
Definition
Pure Alpha agonist. Not a catecholamine (lost –OH at position 4 of benzene ring)
Term
Methoxamine
Definition
Pure Alpha agonist. Not a catecholamine (lost –OH at position 4 of benzene ring)
Term
Oxymetazoline
Definition
Pure Alpha agonist. Not a catecholamine (lost –OH at position 4 of benzene ring)
Term
Amphetamine
Definition
Indirect sympathomimetic. Displaces NE in CNS. Has CNS activity bc lacks –OH at position 3 AND 4 on benzene ring
Term
Metaproterenol
Definition
Selective Beta-2 agonist/bronchodilator. Avoids ^HR that comes with Beta-1/Beta-2 agonists. Ring hydroxyl shifted so COMT inactive -> increased t ½
Term
Terbutaline
Definition
Selective Beta-2 agonist/bronchodilator. Avoids ^HR that comes with Beta-1/Beta-2 agonists. Ring hydroxyl shifted so COMT inactive -> increased t ½
Term
Albuterol
Definition
Selective Beta-2 agonist/bronchodilator. Avoids ^HR that comes with Beta-1/Beta-2 agonists. Ring hydroxyl shifted so COMT inactive -> increased t ½
Term
Dobutamine
Definition
Beta-1 selective agonist. ^CO with less reflex tachycardia (such as with Isoproterenol). Used for CHF
Term
Clonidine
Definition
Stimulates Alpha-2 (feedback inhibitor) receptors in CNS that decrease BP. Used to relieve HTN. Can be used to relieve symptoms of narcotic withdrawal
Term
Phenoxybenzamine
Definition
Irreversible Alpha antagonist (covalent). Receptor can no longer be used. Maximum effect of agonist is decreased
Term
-zosins (Prazosin, Terazosin, Doxazosin)
Definition
Competitive Alpha antagonist/blocker. Alpha-1 selective
Term
Phentolamine
Definition
Nonselective (Alpha-1 and Alpha-2) competitive antagonist
Term
Propranolol
Definition
Prototype of Beta blockers. Beta-1 and Beta-2
Term
Atenolol
Definition
Beta blocker. Cardioselective (Beta-1 only). Excreted only by kidney so t ½ ^^ (high lipophilicity)
Term
Nadolol
Definition
Beta blocker. Not cardioselective. Excreted only by kidney so t ½ ^^ (high lipophilicity)
Term
Metaprolol
Definition
Beta blocker. Cardioselective (Beta-1 only)
Term
Pindolol
Definition
Beta blocker. Partial agonist activity. At rest some ^HR, but w exercise, decreased max HR (~130). Supposedly good for asthmatics but not in reality
Term
Labetolol
Definition
Beta and Alpha blocker. No more effective at decreasing BP than regular Beta-blockers
Term
Esmolol
Definition
Beta blocker with short t ½ (5-10 mins), so used as IV drip to determine efficacy of Beta-blocker in MI patients
Term
Acetylcholine
Definition
PSNS neurotransmitter. Dose for CV< glands/SMC < Ganglia < NMJ (muscarinic). Ganglia< NMJ < CV < glands/SMC (nicotinic)
Term
Muscarine
Definition
Stimulates muscarinic receptors. Use of muscarinics is rare
Term
Nicotine
Definition
Stimulates nicotinic receptors at low doses. Blocks at higher doses (“depolarizing blockade”). Not degraded by AChE. Stimulation then blockade in SNS and PSNS. Only blockade in NMJ (-> resp paralysis)
Term
Bethanachol
Definition
Muscarinic of choice. Used for GI stimulation in hypomotility, treat urinary retention
Term
Atropine
Definition
Anti-muscarinic. Blocks PSNS, used for preanesthetic (dry secretions and constrict airways). Dilates pupils, contraindicated with glaucoma. Mad as hatter, dry as bone, red as beet, blind as stone.
Term
Diphenhydramine
Definition
Antihistamine. Can block muscarinic receptors (classical H1 blockers also block muscarinic receptors)
Term
Histamine
Definition
Vasodilator
Term
Scopolamine
Definition
Antimuscarinic. Oxygen bridge ^CNS penetration. Used for motion sickness.
Term
Ipratropium
Definition
Antimuscarinic. Reduced CNS effects (quaternary amine) make it more desirable than atropine as preanesthetic
Term
Glycopyrrolate
Definition
Antimuscarinic. Reduced CNS effects (quaternary amine) make it more desirable than atropine as preanesthetic
Term
Trimethaphan
Definition
Ganglionic (SNS and PSNS) blocker (nicotinic)
Term
Mecamylamine
Definition
Ganglionic (SNS and PSNS) blocker (nicotinic)
Term
Edrophonium
Definition
Competitive antagonist of AChE. Short duration (10 minutes), so used to test for myasthenia gravis
Term
-stigmines (Neostigmine, Physostigmine, Pyridostigmine)
Definition
Carbamates. Mimic ACh but slow hydrolysis (2-8 hrs). AChE inhibitor used for myasthenia gravis
Term
Parathion
Definition
Organophosphate. Prodrug (-> Paraoxon). AChE inhibitor for mammals and insects. Muscarinic (bronchoconstriction and secretions), nicotinic (paralyze respiratory muscles), CNS (decreased resp drive)
Term
Malathion
Definition
Organophosphate. Prodrug (-> Malaoxon). AChE inhibitor selective for insects, so used as insecticide
Term
Sarin
Definition
Organophosphate. Muscarinic (bronchoconstriction and secretions), nicotinic (paralyze respiratory muscles), CNS (decreased resp drive)
Term
Pralidoxime/2-PAM
Definition
Antidote to organophosphates. Potentiated with atropine (anti-muscarinic)
Term
Ethosuximide
Definition
Blocks T-type calcium channel. Drug of choice for petit mal seizures.
Term
Valproic acid/Divalproex
Definition
Used for petit mal, absence, and tonic-clonic seizures. Hepatotoxic, so do LFTs. Divalproex Na is enteric mixture of valproic acid and sodium valproate to reduce GI upset (GI “seizures”)
Term
Clonazepam
Definition
Benzodiazepine (GABA channel potentiator). Long acting with good efficacy against petit mal seizures. Tolerance will occur
Term
Gabapentin
Definition
GABA channel potentiator (?). Designed as GABA agonist but found to not mimic GABA. Renal excretion. No known significant interactions. Used in combo with other anti-Sz drugs, chronic pain of neural origin
Term
Carbamazepine
Definition
Prolongs inactivation state of Na+ channels. When neuron is firing fast, inactivation is more prominent. Related to tricyclic antidepressants. Drug of choice for partial seizures
Term
Phenytoin
Definition
Hydantoin. Limits spread of Sz in brain. Effective against grand mal and partial seizures. Nonlinear effect and variable between patients. Gingival hyperplasia
Term
Lamotrigine
Definition
Sodium channel inhibitor. Anti-epileptic drug
Term
Topiramate
Definition
“New” anti-epileptic drug, has replaced Phenytoin
Term
Phenobarbital
Definition
Barbiturate. Enhances GABA. Used for grand mal and simple partial Sz. OK for complex partial. May exacerbate petit mal. Tolerance forms to sedative effects but not to anticonvulsive effect (beneficial)
Term
Levetiracetam
Definition
“New” anti-epileptic drug, has replaced Phenytoin
Term
Primidone
Definition
Deoxy barbiturate. Similar to Phenobarbital in uses for epilepsy. Metabolized to Phenobarbital and Phenyethylmalonamide (used for complex partial seizures)
Term
Diazepam
Definition
Benzodiazepine (enhance GABA). Used to treat status epilepticus. Chosen over phenobarbital bc quick onset and decreased effect on respiration
Term
Lorazepam
Definition
Benzodiazepine (enhance GABA). Used to treat status epilepticus. Chosen over phenobarbital bc quick onset and decreased effect on respiration
Term
Memantine
Definition
Antagonist to Glutamate’s NMDA receptor. Used for Alzheimer. Excessive glutamate (-> Ca++) in CNS can lead to neuronal damage
Term
Donepezil
Definition
Cholinesterase inhibitor used for Alzheimer. Keeps patient out of nursing home for several more months
Term
Heroin
Definition
Narcotic. Abused for euphoria and sedative action. OD -> respiratory depression (use Naloxone). Physical and psychological dependence
Term
Methylphenidate
Definition
Indirect-acting sympathomimetic. Displaces NE in CNS. Same effects as cocaine.
Term
Methamphetamine
Definition
Indirect-acting sympathomimetic. Displaces NE in CNS. Same effects as cocaine.
Term
Phenmetrazine
Definition
Indirect-acting sympathomimetic. Current use for narcolepsy and ADHD. Increases BP, HR, arrhythmias, mydriasis. Tolerance occurs to anorexia, euphoria, lethal effects
Term
LSD
Definition
Hallucinogen. No medicinal use, strong psychological dependence, little physical dependence. Small doses produce frank hallucinations. Autonomic effects same as SNS stimulation
Term
Tetrahydrocannabinol
Definition
Hallucinations at high doses (not like LSD – milder). Strong psychological dependence. Metabolites in urine for at least 2-3 weeks.
Term
MDA
Definition
Stimulant and psychedelic effects. Produces degeneration of 5HT in nerve cells and axons in rats. CSF of abusers is low in 5HT metabolites. Abusers get very depressed when they withdraw
Term
MDMA
Definition
Stimulant and psychedelic effects. Produces degeneration of 5HT in nerve cells and axons in rats. CSF of abusers is low in 5HT metabolites. Abusers get very depressed when they withdraw
Term
Phencyclidine
Definition
PCP. Produces numbness, slurred speech at low doses. Analgesia, hallucinations, psychotic states and coma at high doses (bad combo) . Neuroleptics and hospitalization often required.
Term
Methadone
Definition
Narcotic with long t ½. Smaller sedative effect (less reinforcing). Less withdrawal.
Term
Naltrexone
Definition
Opiate blocker. Oral.
Term
L-Dopa
Definition
Crosses the BBB easily. Acts as extra precursor to allow surviving dopamine neurons to increase their output of dopamine. Converted by AAADC/VitB6 to Dopamine. Side effects: psychosis, N/V, arrhythmias
Term
Carbidopa
Definition
Blocks peripheral AAADC. Allows L-Dopa dose to dramatically decrease -> less N/V, fewer arrhythmias, no concerns about VitB6
Term
Pyridoxine/B6
Definition
Cofactor for AAADC. Allows peripheral conversion of L-Dopa to Dopamine. Not preferable, bc L-Dopa is only useful for Parkinson in the CNS
Term
Amantidine
Definition
Antiviral agent that works by increasing dopamine output of nigrostriatal neurons. Parkinson
Term
Selegiline
Definition
Specific MAO-B inhibitor. Does not cause wine and cheese syndrome. Prevents dopamine degradation -> ^levels
Term
Bromocriptine
Definition
Dopamine agonist that can easily cross BBB. Parkinson
Term
Pramipexole
Definition
Dopamine-2 agonist. Can cross BBB. Parkinson
Term
Ropinirole
Definition
Dopamine-2 agonist. Can cross BBB. Parkinson
Term
Entacopone
Definition
COMT inhibitor. Prevents formation of O-Methyl-Dopa (inactive), so more L-Dopa reaches CNS
Term
Chlorpromazine
Definition
Antipsychotic. Phenothiazine derivative. Strong hypotensive and sedative. Strong anti-muscarinic effects. These prevent EPS but give blurred vision, constipation, etc. Low tendency to produce acute dystonia
Term
Haloperidol
Definition
Antipsychotic. Minimal sedation and only mildly antimuscarinic. Associated with high incidence of acute dystonia
Term
Fluphenazine
Definition
“Old” antipsychotic. Dopamine blocker. Not antimuscarinic so no ability to decrease movement difficulties (EPS)
Term
Benztropine
Definition
Antimuscarinic used to treat Parkinson Syndrome (not Disease). Use with Dopamine blockers
Term
Trihexphenidyl
Definition
Antimuscarinic used to treat Parkinson Syndrome (not Disease). Use with Dopamine blockers
Term
Clozapine
Definition
New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Antimuscarinic, hypotensive. Be careful of agranulocytosis
Term
Olanzapine
Definition
New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis
Term
Risperidone
Definition
New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis
Term
Quetiapine
Definition
New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis
Term
Ziprasidone
Definition
New/atypical antipsychotic. Blocks 5HT and all Dopamine receptors. Only mild blockade at D2 so no EPS. Sedative, hypotensive. No agranulocytosis
Term
Aripiprazole
Definition
D2 partial agonist with minimal sedative and hypotensive effects. “Dopamine stabilizer”
Term
Baclofen
Definition
GABA agonist. Spasmolytic. Hyperpolarizes cells and inhibits release of excitatory transmitters. Similar to Diezapam. Sedation a problem
Term
Dantrolene
Definition
Blocks release of Ca++ from sarcoplasmic reticulum. Spasmolytic. Acts peripherally. Major side effect is generalized muscle weakness. Used to treat malignant hyperthermia
Term
Methocarbamol
Definition
Decreases muscle spindle afferent activity (peripheral action) by blocking interneurons. Spasmolytic
Term
Cyclobenzaprine
Definition
Acts in the CNS to decrease repetitive motor activity. Spasmolytic
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