ANS, Neuro, and Psych Drugs Flashcards
Succinylcholine
Depolarizing neuromuscular blocking agent. Keeps nACh channel opens. Giving ache during first phase (fasiculations) potentiates effect AChE during second phase (paralysis) attenuated effect
Pralidoxime
Ach esterase regenerator Used for AchE overdose (eg pesticides) Needs to be given immediately
Carbamates
AChE inhibitors (-stigmines)
Ipatropine
Bronchi relaxation (IPA try to breathe now)
Bethenchol
mAChR agonist Used for postoperative illeus (Beth needs to shit)
Pilocarpine
mAChR agonist Used to induce myosis(pupillary contraction) and for glaucoma (allowing for movement if vit hum out canal of schlem)
Carbachol
mAChR agonist Used for glaucoma (“need to squeeze the eye (constraction) to get rid of extra aqueous humor”) Carborator on pipe to smoke weed another txt for glaucoma
Scopolamine
mAChR antagonist Used as antiemetic (scope to clean out mouth after puking)
Tolterodine
mAChR antagonist Used for urinary incontinence (toltery can hold it man)
Tropicamide
Anticholinergic used to induce mydriasis Tropico is used topically
Tubocurarine Pancuronium
Nondepolarizing paralytic (neuromuscular blocking agent) nAChR antagonist Look for cur as in curare in them
Benzotropine
Anticholinergic fir Parkinson’s Park the Benz (the Benz penetrates the cns)
Atropine
Anticholinergic Antiparkinsonian
Cholomimetic effects?
Cardiac slowing, decreased CO, vasodilation, decreased artery pressure GI peristalsis, contraction of bladder, contraction of bronchial smooth muscle Stim of glands: sweat, lacrimation, salivation and bronchial secretions
Acetylcholinesterase inhibitor overdose?
Overdose= dumbbells Diarrhea urination mitosis bronchochonstriction bradycardia, excitation (of cns-Parkinson’s like; skeletal muscle) lacrimation, salivation, sweating
Anticholinergic effects?
Inhibition of sweat, secretions, tachycardia, mydriasis, cycloplegia, decrease gi motility, relaxation of bronchi biliary and uriniary smooth muscle With kids have to be careful of over activity with hyperthermia and no sweating
Local anesthetics–two classes what are they and how do you know which one is which?
Esters— take away Caine and there won’t be another I in the name Degraded by PABA Amides—take the Caine out and there will be another i These are degraded by cyps
Morphine
Opiate High first pass metabolism, why administered IV
Methadone
Synthetic mu agonist, weaker than morphine and used to help with withdrawal symptoms Cross tolerance exhibited with heroin
Hydromorphone (dilaudid)
Synthetic mu agonist, weaker than morphine and used as alternative Has antitussive effects
Hydrocodone
Oral antitussive and analgesic
Meperidine (Demerol)
Opiate Metabolized to convulsant (therefore renal and hepatic considerations) Tx in hospital until you start seeing fasiculations and then take ptn off of it
Dextromethorphan
Antitussive opiate “Purple drank” robotussin
Diphenoxylate
Antidiarhea formulated with atropine
Loperamide
Antidiarrhea opiate
Naloxone Naltrexone Nalmefene
Opiate antagonists (Tx for OD)
Levodopa
Antiparkinsons DA precursor, passes thru BBB
Carbidopa (sinemet)
Antiparkinsons Decarboxylase inhibitor, given in combo to prevent peripheral breakdown of L dopa. Does not pass into brain Side effects are less than with l dopa alone
Bromocriptine
Antiparkinsons DA agonist Ergot- thus causes fibrosis
Rotigone
Antiparkinsons DA agonist (non ergot) Hits DA R 1,2,3 “Roti does all three”
Ropinirole
Antiparkinsons DA agonist Non ergot If it makes you uncontrollably sleepy then needs to be stopped
Pramiplexole
Antiparkinsons non ergot DA agonist Also used for restless leg syndrome
Apomorphine
Antiparkinsons D4 agonist Need to give antiemetic first
Selegiline Resagiline
Antiparkinsons MAO B inhibitor (B specific for dopamine breakdown) Selegiline has side effects, htn crisis Resagiline does not have side effects
CAN BE USED TO INCREASE DA IN PD
Tolcapone Entacapone
Antiparkinsons COMT inhibitors (Capone!!) Tolcapone has hepatotoxicity Entcapone does not–cuz ents are awesome
CAN BE USED TO INCREASE DA IN PD***** (only effect when used in combo with Levodopa/carbidopa) THESE WORK PERIPHERALLY INCREASING AMOUNT OF LEVODOPA AVAILIBLE FOR BRAIN
Amantadine
Antiviral Antiparkinsons
Antipsychotics
Both work similiarly, you pick drug based on SEs; long half lives; concerned with tardive dyskinesias as SEs—irreversible and immediate stoppage required. Toxicity—parkinsonian effects, SNS effects from muscarinic blockade; also an Alpha adrenergic blockade=postural hypotension and failure to ejaculate, cardiac=prolonged QT Typical (first generation)–D2 antagonists: most have “-zine” cuz the make you zzzzzz -SEs: Extrapyramidal neuro effects (neuroleptic drugs–tranquilizers, bradykinesia, mild rigidity, tremor, akathisia–subjective restlessness) -Also increased release of prolactin–>lacrimation; Dystonias caused by typcals can be relieved via diphenhydramine (benadril) or benzotropine -NB: Haloperidol (haldol), chlorpromazine (thorazine), thioridazine (mellarlil) Atypical (2nd generation): 5-Ht2 antagonists > D2 antagonists; most have “-pine” -SEs: less extrapyramidal symtoms. Do have hypotension, seizures, weight gain, increased risk of type II db, ad hyperlipidemia -NB: Clozapine (clozaril), risperidone (risperdal), paliperidone (invega), olanzapine (zyprexa), quetiapine (seroquel) short half life , ziprasidone short half life, aripiprazole (abilify) Neuroleptic Malignant syndrome: Bromocriptine (ergot DA agonist) and stop antipyshcotic
Chlorpromazine
Typical Antipsychotics–D2 Antagonist; originally called neuroleptic drugs=tranquilizers SEs-Extrapyramidal effects: bradykinesia, mild rigidity, tremor, subjective restlessness (akathisia), reduced initiative and interest, emotional manifestations.
Thioridazine
Typical Antipsychotics–D2 Antagonist; Also has mACh activity which might explain less extrapyramidal effects. Orthostatic hypotension and urinary retention originally called neuroleptic drugs=tranquilizers SEs-Extrapyramidal effects: bradykinesia, mild rigidity, tremor, subjective restlessness (akathisia), reduced initiative and interest, emotional manifestations.
Haloperidol
Typical Antipsychotics–D2 Antagonist; Increased risk for extrapyramidal effect originally called neuroleptic drugs=tranquilizers SEs-Extrapyramidal effects: bradykinesia, mild rigidity, tremor, subjective restlessness (akathisia), reduced initiative and interest, emotional manifestations.
Clozapine (as opposed with Clonidine)
Clozaril; Reduced risk of extrapyrmaidal effects, saved for tx resistant psychosis, works well but risk of agranulocytosis (monitor blood counts) Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia (clonidine: central alpha 2 agonist which decreases SNS tone in HTN)
Clozapine (as opposed with Clonidine)
Clozaril; Reduced risk of extrapyrmaidal effects, saved for tx resistant psychosis, works well but risk of agranulocytosis (monitor blood counts) Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist (WORKS ON D4 agonists as welL) SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia (clonidine: central alpha 2 agonist which decreases SNS tone in HTN)
Paliperidone
Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia
Olanzapine
Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia
Quetiapine
Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia
Ziprasidone
Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia
Aripiprazole
Abilify Atypical Antipsychotic–5-ht2 antagonists and D2r antagonist SEs-Seizures, hypotension, weight gain, increased risk for type II db, and hyperlipidemia
Anxiolytic Drugs
Sedative agent reducing anxiety and exerting a calming effect; can be hypnotic (sleep promoting); lipophillicity will determine CNS penetration; Cyp 3a4 then glucoronidation; many metabolites will have very long half lives therefore need to considerhepatic dysfunction and age (older ppl give less); instruction patients not to drive or drink or take anticholinergerics or antihistamines, HIGH RISK OF DEPENDENCE–don’t write refills so they cannot horde them (suicide) and need to check up with you; can have anterograde amnesic affects. always short term use of sedatives (except things like Generalize anxiety disorder, panic disorder agroaphobia which can be longer use) Can have withdrawal where you need to wene them off and/or psychological dependence; FLUMZAENIL for BZ OD competitive inhibitor with SHORT half life Benzodiazepines–much safer as with large doses only cause anesthesia and not coma or respiratory depression; GABAa agonists (2 spots on channel) causing increased opening frq, not duration per opening; ANTICONVULSANTS (not barbs); muscle relaxation, slight resp depression only concerned with a pulmonary patient MOST END IN “AM” Barbituates–can causes coma with large doses, abuse and fatal potential; binding site inside of pore, therefore influences how long it stays open not freq of opening “-tal” NB Can give B-adrenergics to block peripheral effects of anxiety, will not remove subjective feeling however.
Lorazepam
Benzo: Ativan Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Clonazepam
Benzo–Kloniopin Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Chlordiazepoxide
Benzo: Librium Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Oxazepam
Generic Benzo Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Clorazepate
Tranxene Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills
Diazepam
Benzo–Valium Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Alprazolam
Benzo: Xanax Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Midazolam
Benzo: Versed Benzodiazepine Long half life, no active metabolites Instruct patient not to drive, use alchol, anticholinergics, or antihistamine. No refills Tx: Acute Anxiety states, panic attackes, generalized anxiety disorder, insomnia, skeletal muscle relazation, seizure disorders
Phenobarbital
Long acting Barbituate - Most commonly used drug for seizure disorders Binds inside of Gaba channel–increase duration of opening (as opposed to benzos increasing frequency) Induces Cyp450s–will stop birth control from working Depletes vit k, d and folate
Pentobarbital
Barbituate Binds inside of channel
Buspirone
NON BENZO Anxiolytic: BuSpar Longer onset, fewer side effects
Flumazenil
Benzo ANTIDOTE with Short half life (will not work with Barbiutate overdose)**** Romazicon BZ binding site antagonist with VERY short half life. Used for BZ OD but need to give every few hours while you wait for person to clear system of BZ
Reserpine
Anti-serotoninergic, originally used as an antihypertensive Prevents uptake of 5ht into vessicles
Antidepressants
Need to tx for several weeks, monoamine neurotransmission hypothesis Reuptake blockers: -SSRI’s -SNRI’s–Blocks uptake of 5-ht and NE -TCA’s–Non Selective reuptake inhibitors Metabolism inhibitors -MAOI’s (A=nonspecific, NE and 5-HT, tyramine) (MAOs tend to be in presynaptic terminal, while COMTs tend to be on post-synaptic cleft); cause HTN particularly with Tyramine (fish, cheese)**** SARI’s–(serotonin antagonist and reuptake inhibitor) –Not well understood since two effects seem counterproductive, explanation is that they selectively do this
Trazodone
SARI–serotonin Antagonist and reuptake inhibitor Causes Sedation via histamine blockage 2nd Gen SARI’s–(serotonin antagonist and reuptake inhibitor) –Not well understood since two effects seem counterproductive, explanation is that they selectively do this Prodrug,
Nefazodone
SARI. Heptatoxicity 2nd Gen SARI’s–(serotonin antagonist and reuptake inhibitor) –Not well understood since two effects seem counterproductive, explanation is that they selectively do this Structural anaolgo of 5-ht, antagonist for 5-ht2a/2c and 5-ht3
Mirtazapine
SARI. Sedation. Weight gain (attractive for elderly) 2nd Gen SARI’s–(serotonin antagonist and reuptake inhibitor) –Not well understood since two effects seem counterproductive, explanation is that they selectively do this Structural anaolgo of 5-ht, antagonist for 5-ht2a/2c and 5-ht3
Bupropion
Antidepressant (in a class by itself), Smoking Cessation, Welbutrin; “Mom should be ON bupropriON” Enhances both NE and DA transmission while inhibiting reuptake of NE and DA Don’t use with eating disorders (bulimia) due to seizure risk
MAJOR SIDE EFFECT IS SEIZURES
SSRIs
Blocks 5ht transporters Tx for MDD, Anxeity disorder, ocd, pmdd, ptsd, bulimeia etc. Sexual dysfunction, sleep issues
Fluoxetine
SSRIs–Prozac
Paroxetine
SSRI—Paxil Teratogenic–No pregnancy (3 P’s)
Sertraline
SSRI Zoloft
Citalopram
Celexa - SSRI
SNRIs
Reuptake for NE and 5ht (little DA) Antidepressant (backup for SSRIs), Sympathetomemmitcs**** + Anticholinergic, sedation, hypertension (particularly Venlafaxine) <—from NE
Venlafaxine
SNRI - Effexor Hypertension
Duloxetine
SNRIs - Cymbalta
Tricyclic Antidepressants
Blocks NE and 5-ht less selective than SNRIs: Also blocks alpha adernergic receptors (HYPOTENSION**** compared with SNRIs=HTN), antihistamine (sedation) Overdose: arrhythmias/seizures
OD FROM ARRYTHMIAS from blocking fast Na channel in cardiomyocytes
Impipramine
TCA
Amitriptyline
TCA Antidepressant; amiTRItiptine=TRIcyclic
Clomipramine
TCA antidepressant—Anafranil
MOAI’s
Tx for Major Depression unresponsive to other drugs HTN Crisis with TYRAMINE–(w/ meats and cheese) or Sympathomimetics Serotonin syndrome with SSRIs Tox: Hypotension and insomnia
Phenelzine
MAOI-A Antidepressant Inhibits breakdown of NE, DA and tyramine HTN CRISIS with tyramine containing food (cheese, meat)
Selegiline
MAOIBs
Lithium
Mood stabilizing drug used as Bipolar Treatment Enters via Na+ channel, 6 to 8 hour half life, Low therapuetic index: 0.6 to 1.4 mEq/L target range; 2=toxicity Diuretics DECREASE clearance about ~25% SE is tremor which is controlled by propranolol or atenolol, decreases thyroid function, polydipsia and polyuria Not used in Dehydration, hyponatremia, significant CVD or renal impairment
Doxepin (Silenor)
Insomnia Tx: Potent H1 Blocker
General Anethestics
IV for Induction Inhaled for Maintence Benzos for amnesia Opioids for using less inhaled and for post op analgesia neuromusclular blocking drug to prevent patient moving during procedure Inhaled= MAC–minimum alveolar concentration (measure of potentcy). Less soluable has faster onset (it fills the well faster) Effect–decreases BP (vasodilation and negative inotropy), increased Resp Rate and lower tidal volumes (causing lower minute volume). Concerns with Malignant hyperthermia–decreased reuptake of Ca2+ from sarcoplasmic reticulum causing increased temp and muscle contractions. Tx with Dantrolene (inhibiting release from Sarcoplasmic reticulum) IV=method of induction (fast on/off), lipiphillic going first to highly perfused tissues and then washing out fast; context specific half life time
Datrolene
Antidote for malignant hyperthermia. Inhibits release from sarcoplasmic reticulum
NO
Inhaled Anesthetic Used as adjunct for amnesia and has analgesic actions
Isoflurane, Sevoflurane, Desflurane
Volatile Inhaled Anesthetics Sevoflurane is the most pleasant to inhale and used for induction of kids Iso>Sevo>Des (least soluable thus better (Lower) MAC=minimum alveolar concnetration)
Propofol
IV anesthetic “MJ Juice, Milk of amnesia” Used as induction agent Vasodilatory and negative inotropy, decreases tidal volume, RR and minute volume, decrease in upper airway reflexes antiemtic
Etomidate
IV Anesthetic Use with Cardiovascualry comprimised patient (no hemodynamic effects: HR, BP, inotropy) Non-analgesic, Respiratory depressant, associated with PONV (post op nausea and vomitting)
Ketamine
IV Anesthetic Airway reflexes are preserved in most situations, secretions/lacrimations are increase, hallucinations and upleasant emergence might occur (suggested benzo co-administration) sub-analgesic doses might help in limiting or reversing opioid tolerance (effectively lowering the therapuetic doses necessary for opioids)
Dexmedetomidine
IV Anesthetic Used for sedation or adjunct to general anesthetic, and analgesic Significant deceases in BP/HR (to the point you need to give atropine sometimes) Mechanism of action: Alpha 2 agonist in LC and SC Good cuz preserve respiratory drive, context sensitive half life significantly increases after 8 hours of infusion
Antiepileptics
3 Mechanisms of action: 1) Decrease Glutamate 2) Increase GABA 3) Modify Na/Ca Conductances Partial Seizures: Phenytoin, Carbamazepine, Valproate Generalized Tonic-Clonic (grand mal): Phenytoin, Carbamazepine, Valproate Absent (petit mal Seizures): Ethosuximide, Valproate (clonazepam) Myoclonic Seizures: Phenobarbital, Valproate (Clonazepam) Status Epilepticus: Phenobarbital, Diazepam (REALLY YOU WANT THEM UNDER GENERAL ANESTHESIA)
Phenytoin
Anti-Epileptic: Cyclic Ureide. Blocks Na channels, and thus decreasing glutamate. Phenoyt ion makes you face look funny Use for Generalized Tonic clonic and partial seizures SEs: Nystagmus diplopia, sedation, hirustims, anemisa peripheral neuropathy,osteoporiss, induction of hepatic drug metabolismo Important: Teratogenic (cleft lips/palates), induces Cyp450s thus birth ctl won’t work, hirutism, coarsening facial features and nystagmus associated, GINGIVAL HYPERPLASIA, Megaloblastic anemia,
Ethosuximide
Anti-epileptic used for absence seizures; slows T-ca2+ channels in thalmus. Causes nausea Succinimide anticonvulsant, used over valproic acid (valproate) dt no hepatotoxic effects
Valproate
Broad spectrum antiepileptic, most effective for myoclonic/atonic; Decreases T-caclium channel activity, hepatotoxic, increases gaba concentration in brain Used for generalized tonic-clonic, parital nd myoclonic siezures. Teratogenic and potential hepatotoxic (infants) SEs: Drowsiness nausea, tremor, hair loss ,weight gain, inhibition of heaptic drug metabolism
Carbamazepine
Anti-epileptic, and Mood stabilizer (BP) and antipsychotic agent for schizo. Also trigemneal neuralgia Inhibts votlage gated Na channels decreasing synaptic release of glutamate SEs: AGRANULOCYTOSIS AND APLASTIC CRISIS; Diplopia cog dysfunction, drowsiness, ataxia. Teratogenic potential and rare for steven johnson syndrome (life threatening skin condition causing the epidermis to separate from dermis—thought ot be a hypersensitivity Rxn)
Lamotrigene
Antiepileptic Toxic-epidermal necrosis (Stevens-Johnson syndrome) Prolongs inactivation of Na channels
Dementia Txs
AChEI’s and NMDA’s Receptor Antagonists
Donepazil, Rivastigmine, Galantamine
Dementia Txs: AChEI’s
Mementine
Dementia Tx: NMDA receptor antagonists (protects against glutamate excitotoxicity)
Drug used to prevent cerebral vasospasm following stroke?
Nimodipine (Calcium channel blocker)
Most common cause of bacterial meningitis in adults?
Lancet Gram positive Cocci in pairs (strep pneumonia)
