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D&T 2: Exam 2 > Druhgs > Flashcards

Druhgs Flashcards

1
Q

CYP2D6

A

Hepatic Enzyme that catalyzes the conversion of codeine to morphine

  • Strong allele =» Codeine is toxic due to increased conversion
  • Weak allele =» Codeine is ineffective analgesic
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2
Q

Hydromorphone

A

Derivative compound of morphine that is used for VERY SEVERE pain

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3
Q

Methadone

A

Effective analgesic that is as effective as morphine but has a much longer half-life and better bioavailability; no kappa activity

⭐️Assoc. With biliary spasms

-Drug has less incidence of tolerance and is used to treat addiction thru “Methadone Maintenance”- administration of methadone leads to the satisfying of craving needs w/o morphine use; does not reach the same relative high and lasts much longer (only need to take once a day)

Yeah methadone maintenance should probably be it’s own card but fuck you future michael

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4
Q

What is the urinary metabolite of heroin?

A

6-monoacetylmorphine

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5
Q

Meperidine

A

Synthetic derivative of morphine that serves as a u-agonist; causes CNS excitement at toxic doses due to metabolite and cannot be corrected by naloxone

-Can also develop tolerance (slowly) and dependence but has better bioavailability

**Use w/ MAOIs =»delirium, hyperpyrexia, convulsions

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6
Q

Fentanyl

A

u-opiod agonist that is much more potent than morphine and acts much faster; mixed w/ some batches of heroin

-Is a synthetic derivative of morphine

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7
Q

Morphine

A

Acts strongly on u receptors and weakly on k receptor; prevents the release of substance P and acts on respiratory centers, pain perception, and mood/emotion

Uses: Gold Standard tx for moderate-severe pain; pulmonary edema; pre-surgery anesthetic

-Causes analgesia w/o loss of consciousness along with euphoria

**Will see pathognomic miosis due to activation of the Edinger-Westphal nucleus; other major adverse effect is respiratory depression due to decreased neural sensitivity to CO2

-Possible constipation can occur; rebound syndrome will occur from all of these listed side effects as well

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8
Q

Buprenorphine

A

Partial u-agonist/k-antagonist; approved for the treatment of opioid dependence

***Used for pregnant drug addicts

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9
Q

Tramadol

A

5-HT and NE reuptake-inhibitor that also binds to opioid receptors for some bullshit reason; used for moderate pain, potential for abuse because its given to dogs and people take it

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10
Q

Naloxone/Naltrexone

A

Opioid antagonists used to reverse opioid poisoning and also to prevent dependence; will induce immediate withdrawal

Naltrexone is also approved for use in alcoholism

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11
Q

Clonidine

A

Alpha-2 adrenergic that inhibits pain in the dorsal horn projection neurons

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12
Q

Baclofen

A

Use: Spasticity of muscles (usually lower back); works on GABA-B receptor to inhibit motor neurons

-Can induce CNS depression, psychiatric sx, weakness, and comes w/ a BLACK BOX WARNING
=»Abrupt withdrawal causes severe sequelae including hyperpyrexia, rebound reflexia/spasticity, muscle rigidity- all of which can cause organ failure and even death

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13
Q

Carisoprodol

A

Uses: Acute MSK pain

Has anticholinergic activity

Do not use in pts. Under 16 or in pts. W/ potential for abuse

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14
Q

Cyclobenzaprine

A

Uses: Acute muscle spasms, pain, and **TMJ

ADR: Similar to TCAs so use same precautions (prevent SS); do not use in elderly; can cause anti-muscarinic side effects

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15
Q

Metaxalone

A

Uses: Muscle Discomfort

ADR: Jaundice, CNS depression, do not use w/ renal impairment

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16
Q

Tizanadine

A

Uses: Tension headache, muscle spasticity,

a2-adrenergic agent that acts on the spinal cord

ADRs: Use w/ care in elderly or pts. w/ contraceptives; causes a2-adrenergic side effects (hypotension, bradycardia, weakness)

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17
Q

Plasma Kinin System

A

HMWKG is converted to bradykinin via plasma kallikrein

***Plasma prekallikrein is activated by Factor XIIa; kallikrein will then also activate more Factor XII

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18
Q

Tissue Kallikrein System

A

Tissue Kallikrein converts LMWKG to kallidin

Kallidin is then converted to bradykinin via aminopeptidase

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19
Q

Kininase I

A

Carboxypeptidase N and M; cleaves kinins into ACTIVE metabolites

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20
Q

Kininase II

A

ACE; converts bradykinin into an INACTIVE metabolite

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21
Q

B1 Kinin Receptor

A

Activated by Bradykinin and its metabolites; expression is induced by inflammation

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22
Q

B2 Kinin Receptor

A

Activated by native Bradykinin and kallidin; constitutively expressed

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23
Q

CGRP

A

Calcitonin Gene Related Peptide; most potent vasodilator of the trigeminal system

-Excess release causes migraine

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24
Q

Rate-limiting step of 5-HT synthesis

A

L-tryptophan conversion to 5-hydroxytryptophan BY Typtophan hydroxylase

(then converted to 5-HT by L-AAD

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25
Q

5-HT receptors (1D and 1B)

A

1D =»induces vasoconstriction of cranial blood vessels

1B =» Inhibits nociceptive trigeminal afferents; big role-player in migraine tx

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26
Q

Prophylactic Tx of Migraines and side effects

A

Propanolol (b-blocker): unknown mechanism; avoid use in COPD pt.

Amitryptilline (TCA): inhibition of serotonin uptake?; may cause fatigue

Valproic Acid, Topiramate, Gabapentin (anticonvulsants): Increases in GABA
***Valproic Acid is a NONO in pregnancy

Verapamil (Ca-blocker): decreased inotropy and HTN possible

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27
Q

Abortive Migraine Drugs

A

Mild: NSAIDs

Moderate: Ketorolac; only use for 5 days or else will cause GI damage

Children: No aspirin

Preggers: NSAIDs ok until 3rd trimester

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28
Q

Ergot Alkaloid Mechanism and Side Effects

A

Agonists at 5-HT receptors and partial antagonists at serotonergic, adrenergic, and dopaminergic receptors

ADRs: N/V
Generalized vasoconstriction
Pregnancy X drug (causes miscarriage)

-Also should not use alongside triptans

⭐️DO NOT USE IN PREGGERS, ISCHEMIC HEART DISEASE, ORMPERIPHERAL VASCULAR DISEASE

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29
Q

Triptan mechanism

A

Selective 5-HT agonist; causes less side effects than ergot alkaloids

Cause vasoconstriction of cranial blood vessels, reduction of trigeminal neuron activation and decreased peptide release, and inhibition of NT release in the brainstem

***AVOID use w/ SSRIs =» Serotonin Storm (restlessness, loss of coordination, diarrhea)

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30
Q

Sumatriptan

A

Short onset and duration of action; very short plasma t^1/2

-Relief only for about 2 hrs

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31
Q

Naratriptan and Zolmitriptan

A

Given orally and has better bioavailability and longer duration of action than sumatriptan

-Lower dose for renally impaired pts.

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32
Q

Flovatriptan

A

Longest acting triptan w/ highest affinity for 5-HT1B receptor BUT has long onset of action

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33
Q

Rizatriptan (sounds like eliza)

A

Quick dissolving sublingual tablet w/ a faster onset of action and les N/V than sumatriptan

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34
Q

Timeline of neuroleptic therapy

A

1-3 days: Decreased agitation, aggression, and anxiety; seems to be at normal behavior

1-2 weeks: Increased socialization, self-care, and mood

3-6 weeks: Decreased delusions/hallucinations, appropriate conversations

*Relapse is common if therapy discontinued

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35
Q

Haloperidol

A

Typical neuroleptic drug that is also used to treat Huntington’s Tourette’s

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36
Q

Chlorpromazine

A

Phenothiazine typical neuroleptic that is used for hiccough but is contraindicated in pts. w/ seizures

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37
Q

Thioridazine

A

Typical neuroleptic that deposits in the retina at high conc.

***Cannot be used as an anti-emetic as well as aripiprazole

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38
Q

Extrapyramidal side effects of neuroleptics

A

Exhibited by typicals but NOT atypicals

  • due to their preferred action at the mesocortical pathway and not the nigrostriatal
  • typicals also act on Mesolimbic pathway to treat positive sx
  • Produces dystonias and pseudoparkinsonism
  • Treat w/ removal of drug and anticholinergic like biperidin
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39
Q

Tardive Dyskinesia

A

Develops months/years after tx w/ neuroleptics due to hypersensitivity of DA receptors; incidence is very low w/ clozapine (atypical)

Presents as involuntary facial movements

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40
Q

Neuroleptic Malignant Syndrome

A

Potentially fatal condition that presents w/ muscle rigidity, hyperthermia, tachypnea, and tachycardia; common w/ typical neuroleptics

***STOP Tx IMMEDIATELY; administer bromocriptine (D2 agonist) and dantrolene

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41
Q

Prolactin and Neuroleptics

A

Excessive secretion can occur due to blockade in the tuberoinfundibular pathway; most common w/ phenothiazines

-Produces issues w/ compliance

42
Q

Cholinergic effects of neuroleptics

A

Dry mouth, blurred vision, urinary retention, constipation

-Thioridazine, Chlorpromazine, Olanzapine, Clozapine (no dry mouth tho)

43
Q

Metabolic Side effects of neuroleptics

A

Most common w/ atypicals (especially clozapine, olanzapine) but also significant w/ chlorpromazine

-Potential leukopenia w/ clozapine

Risperidone =» slight weight gain

Haloperidol =» possibly nothing

44
Q

Rabbit Syndrome

A

Perioral tremor assoc. w/ longterm use of neuroleptics

-Tx w/ anticholinergic antiparkinson drugs

45
Q

Contraindications to Neuroleptics

A

***Pregnancy

-Amphetamine use, anticholinergics (worsens extrapyramidal sx), SSRIs, antihypertensives

46
Q

Opiod Abuse

A

Mechanism: Increased dopamine release in the nucleus accumbens =» euphoria

OD: Respiratory depression, miosis, constipation

Maintenance: Treat respiratory sx in OD and possible naloxone; methadone maintenance and buprenorphine possibilities for termination of addiction

Withdrawal: Pupil dilation, diarrhea, yawning, myalgias, dysphoria

47
Q

Benzodiazepine abuse

A

Mech: Depressant?

OD: Supportive care unless coupled w/ other depressants like alcohol; then use flumazenil

Withdrawal: Tremors, dysphoria, seizures (possible)

**Flunitrazepam= Roofies in the Hangover (date rape drug)

48
Q

Propofol

A

Anesthetic that is safe in clinical settings, however, is currently being abused by anesthesiologists in order to get “power naps”

-Leads to addiction w/ chronic use

49
Q

Amphetamine Abuse

A

Mech: Increase NT by DA, NE, and 5-HT; also blocks the reuptake of these NTs and inhibits MAO
=»Increased attention (good for ADHD), euphoria, mood, and decreased appetite

Chronic Use can induce shizophrenic like state or convulsions alongside agitation and restlessness

  • Also causes Meth Mites and Meth Mouth
  • **Tolerance can occur to euphoric effects BUT NOT CNS EFFECTS

OD: Tachycardia, mydriasis, hyperthermia
=» Tx is benzodiazepine and possibly antipsychotics (chlorpromazine, haloperidol)

Withdrawal: Hunger, Mental Depression, Fatigue

50
Q

MDMA

A

Amphetamine derivative that increases 5-HT levels; causes increased euphoria with heightened sexuality and hallucinations that can last up to one week

OD: Hyperthermia, arrhythmia, convulsions, psychosis and depression in long term

51
Q

Cocaine Abuse

A

Mech: Blocks reuptake of NE, DA, 5-HT ultimately leading to their depletion and the need for chronic use
-Also blocks Na+ channels making it a good topical anesthetic

OD: Weak, rapid pulse w/ tonic-clonic seizures and cardiac arrest due to irregular heartbeat and irregular SV

Tx: Benzodiazepine; CANNOT USE B-BLOCKERS (like propanolol)

  • Will potentiate MI and HTN effects
  • Bromocriptine possible to treat addiction
52
Q

Cocaethylene

A

Cocaine and alcohol metabolic byproduct capable of crossing the BBB and being just as potent as cocaine

53
Q

Levamisole

A

Used to cut cocaine and induce stronger effects; can cause agranulocytosis and neutropenia

54
Q

Bath Salts

A

Combination of mephedrone, MDPV, and methylone that produce similar effects of amphetamines but not as potent

  • Causes euphoria and appreciation of arts
  • Tx is similar to amphetamines
55
Q

Nicotine

A

Mech: Initially activates and then blocks cholinergic nicotinic receptors; inhibits MAO to increase DA neurotransmission causing dependence
=» mild euphoria, increased memory, metabolism

-Major metabolite is cotinine after being metabolized in liver (ehh)

Withdrawal: Peaks after 1-2 days but will then start to get better (irritability, anxiety, headaches)

-When pt. says smoking calms them down, they are actually going thru withdrawal sx

56
Q

Caffeine (Methyxanthine)

A

Mech: Inhibits PDE causing an increased cGMP and cAMP; clinically used for acute cardiac failure, diuresis, and possible relief of spinal tap headache

-Will also increased gastric HCl so do not give to gastric ulcer pt.

Uses: idiopathic apnea of prematurity, spinal tap headache, acute cardiac failure

57
Q

Lysergic Acid Diethylamide

A

5HT-1 agonist that serves as a hallucinogen w/ brilliant colors and mood elevation; haloperidol can block hallucinations

58
Q

Mushrooms

A

Utilizes psilobycin to produce hallucinations but causes mydriasis, confusion, vertigo, N/V

-Tx w/ diazepam

59
Q

Ketamine

A

Used to promote dissociative anesthesia; chemically related to PCP and fnxns by blocking the NMDA receptor

-Has little utility due to recovery hallucinations and irrational behavior

60
Q

Anesthesia stages

A
  1. Analgesia; pt. is conscious and conversational
  2. Excitement; pt. has tachycardia, tachypnea, HTN, mydriasis
    • Goal is to limit this stage w/ short acting barbituate (Thiopental)
  3. Surgical Anesthesia; regular respiration and muscular relaxation
  4. Medullary paralysis; this is bad
61
Q

Localized Anesthetics

A

Includes esters (benzocaine, cocaine) and amides (lidocaine, bupivecaine, mepivacaine); works by binding to Na+ channels and inhibiting the nerve conduction

Produces loss of: Pain, temperature, touch (stop here), sympathetic vasomotor activity, skeletal tone; nerves recover in reverse order

ADRs: CNS effects; hypotension
***Hypersensitivity w/ esters due to metabolism of these drugs to PABA

62
Q

Vasoconstrictor effect on anesthetics

A

Prolongs the effect of anesthetics by slowing the absorption and decreasing the amnt of side effects

63
Q

Topical anesthetic for skin

A

Benzocaine

64
Q

Bupivacaine

A

Injected into the epidural space of pts. in labor and it is then absorbed into systemic circulation

-Prevent cardiac depression and CNS toxicity

65
Q

Autonomic Nervous System of the Eye

A

a1 receptors =» iris dilator, Mueller muscle

B2 =» Ciliary muscle

Muscarinic =» Iris sphincter, ciliary muscle

66
Q

Phenylephrine

A

a1 agonist that induces mydriasis; commonly used in optho office for examinations

  • Will maintain pupillary light reflex; often used in conjunction w/ tropicamide, a cholinergic antagonist
  • 10% phenyl sometimes used for uveitis
67
Q

Aproclonidine

A

Selective a2 agonist that decreased aqueous humor production and increases outflow; used in office for the rapid reduction of severe high IOP

  • Loses its efficacy w/ prolonged use
  • Go-to for pre-op laser surgery

-Can also be used to diagnose Horner’s
=» WILL CAUSE PUPIL DILATION (typically this test is used instead of cocaine)

68
Q

Brimonidine

A

***GO-TO for NTG; highly selective for a2 receptors

69
Q

Cocaine Opthalmological Use

A

Used to diagnose Horner’s Syndrome

=»In a Horner’s eye, you will see no dilation after administration (due to the nerve having altered NE receptors)

70
Q

Hydroxyamphetamine

A

Used to diagnose what TYPE of Horner’s is present; causes excess release of NE from the pre-synaptic terminals of post-ganglionic neurons to the dilator muscle

  • No dilation =» POST-GANGLIONIC HORNER’S
    • is less serious; could be assoc. w/ Goiter

-Pre-ganglionic could be assoc. w/ lung tumors or aortic aneurysm

71
Q

Dapiprazole

A

Reverses mydriasis; competitively binds to postsynaptic receptors of the iris dilator muscle

72
Q

Timolol

A

Topical B-blocker used to treat glaucoma; blocks B-receptors =» reduction in aqueous humor production

*Non-selective so contraindicated in CHF or COPD pts.

73
Q

Betaxolol

A

B1 selective blocker that is less potent than Timolol but is ok to used in COPD pts.

74
Q

Carteolol

A

B-blocker w/ intrinsic sympathomimetic activity; competes for B-adrenergic receptors and only has limited activity when it does bind

-No selectivity

75
Q

Pilocarpine

A

***Used to treat acute angle closure glaucoma

-Works by inducing miosis and activating the constrictor muscle

76
Q

Carbachol

A

Causes longer lasting miosis than pilocarpine and can be used in cataract surgeries

77
Q

Homatropine

A

Cholinergic antagonist that Produces great mydriasis and cycloplegia

***Used to reduce pain in uveitis

78
Q

Atropine

A

Cholinergic antagonist that has THE BEST mydriasis and cycloplegia

***Used in eye exams for children BUT CANT USE IN DOWN SYNDROME PATIENTS

79
Q

Cyclopentoate

A

Cholinomimetic drug that is used as a mydriatic in pediatric ocular examination

80
Q

Neurology of ADHD

A

Impusilveness/Hyperactivity- Alterations within the orbitofrontal complex

Inattentiveness- Alterations in the dorsolateral prefrontal cortex and the dorsal anterior cingulate cortex

81
Q

Treatment of ADHD

A

Methylphenidate (RITALIN, Concerta, Daytrana)- inhibitor of NE and DA reuptake; has increased euphoria, attention, decreased appetite =» potential for abuse

Amphetamines

Atomoxetine- Selective NE reuptake inhibitor; **non-stimulant so has lower abuse potential but avoid MAOIs and CVD pts.

Clonidine/Guanicine- good for reducing aggression

82
Q

Treatment of Oppositional Defiance Disorder and Conduct Disorder

A

ADHD Medications- (Ritalin, Amphetamines, Clonidine)

Mood stabilizers- Lithium, VA

Anti-psychotics- Risperidone, apripazole

83
Q

Treatment of Autism Spectrum Disorders

A

Inattention and Hyperactivity- ADHD, anxiety drugs (SSRIs, risperidone)

Disruptive behavior- Risperidone, SSRIs, atypical neuroleptics, clonidine

Repetitive Behavior- Fluoxetine, Risperidone

84
Q

Tourette’s Neurology

A

Likely due to disinhibition of the cortico-striatal-thalamic cortical loop causing increased activity of the caudate nucleus

85
Q

Treatment of Tourette’s

A

Tics- Atypical antipsychotics (D2 agonists, Fluphenzaine, Pimozide), Tetrabenazine, Botox

Behavioral sx- Clonidine, SSRIs

86
Q

Status epilepticus

A

Generalized tonic-clonic seizures so frequent that another seizure begins before the post-ictal phase for the previous one ends; causes hypoxia of the brain making it a potentially fatal medical emergency

Tx: IV Benzos (lorazepam, diazepam) followed by IV Phenytoin to prevent seizure from recurring

-If refractory, give more

If still refractory, give phenobarbital or propofol (no preference)

87
Q

Phenytoin (A)

A

Mechanism: Blockade of Ca2+ influx and enhances Cl- mediated IPSPs (prevents spread)

  • Initial DOC in all epilepsy except Absence and atonic
  • Given orally or in IV if status epilepticus; operates under zero order kinetics and saturates enzymes at therapeutic range

ADRs: Gingival hyperplasia (kids), Stevens-Johnson, Hirsutism, Nystagmus, Possible aplastic anemia
-Also causes birth defects and should not be used in CV pts.

Metabolism: Enhanced by carbamazepine; induces CYP3A4 causing decreased Digoxin, steroids, and Vitamin K (may need supplements)

88
Q

Carbamazepine (A?)

A
  • First line drug for trigeminal neuralgia
    • Also used for generalized tonic clonic and complex partial (2nd line)
  • Can make myoclonic seizures worse

***Autoinduces its own metabolism =» t^1/2 in the blood will decrease after continued administration

89
Q

Phenobarbitals (in epilepsy)

A

Mechanism: Enhances GABA-mediated Cl- flux into cells

  • Used in complex partial, Grand mal, and febrile seizures
    • Mostly used in infants

-Has an additive effect w/ other CNS depressants; can also cause severe respiratory depression (medullary depression)

**Valproic Acid decreases its metabolism (increased blood levels)

90
Q

Valproic Acid (B)

VALPO-FLAKES

A

Mech: Interacts w/ GABA-ergic neurons enhancing depolarizing effects and blocks Na+, K+, and T-type Ca2+

Uses: Myoclonic seizures, Absence seizures refractory to ethosuximide, and Bipolar disorder
-Also combination therapy for other seizures

ADRs: Alopecia, hepatic failure, hematologic dysfnxn

  • **AVOID in pts >2 and hemophiliacs
  • **ALSO AVOID IN PREGGER PTS. =» Babies w/ polydactyl, cleft palate, spina bifida

Inhibits P450s causing increased conc. of other antiepileptics; especially Phenytoin

91
Q

Ethosuximide

A

Mech: Blocks t-type Ca2+ channels of thalamic interneurons

Uses: ABSENCE SEIZURES (guess what pathways are interrupted in them)

92
Q

Lorazepam, Diazepam, Clonazepam (antiepileptics)

A

Mech: Bind to GABAa receptor promoting its fnxn

=»Abrupt withdrawals can cause rebound seizures

93
Q

Lamotrigine (A,C)

A

Mech: Inhibits voltage sensitive Na+ channels and inhibits glutamate release

Uses: Generalized, atonic, absence, **add-on for Lennox-Gastaut

ADRs: STEVENS-JOHNSON (DO NOT GIVE TO PTS. >16 y.o.)
-Highest probability of all antiepileptics

Metabolism: Induced by phenytoin and carbamazepine; inhibited by VA
-Also induces its own metabolism, important to do work-up for this drug

94
Q

Topiramate (antiepileptic)

A

Mech: Inhibits Na+, AMPA, and potentiates GABA effects

Uses: Adjunct usually, but good for pts. w/ refractory tonic/clonic
-Also can be used in Lennox-Gastaut if pts. older than 2

ADRs: ***Kidney stones, CA inhibitor (possible IIH drug)

95
Q

Levetiracetam

A

Used as an adjunct usually but is good for pts. w/ bad livers; will help the liver metabolize potentially damaging drugs

96
Q

Oxcarbazepine

A

Mech: Blocks voltage-gated Na+ channels

Uses: Partial seizures, medication resistant epilepsy

ADRs: Hyponatremia for the first 3 months

97
Q

Fetal Hydantoin Syndrome

A

Baby born with congenital heart disease, cleft palate/lip, mental deficiencies due to teratogenic properties of phenytoin

=»Avoid by planning the pregnancy in an epileptic, providing Folic acid, and switching pt. from phenytoin and barbiturates to something else

  • If pregnancy was unplanned, DO NOT SWITCH; just try to use the lowest dose possible
    • Possible rebound seizure will produce anoxia and damage baby
98
Q

Prochlorperazine

A

Typical antipsychotic given during chemo because it is an effective anti-emetic

99
Q

When can you consider opioid detoxification for a pregnant patient?

A

If pt. Is taking less than 40mg a day and the fetus is less than 20 weeks old

100
Q

Longest lasting pain reliever on the market

A

OxyContin

-Hillbilly heroin

101
Q

What drug is safe to use to produce Mydriasis and cycloplegia in glaucoma patients?

A

Tropicamide- a Cholinergic antagonist with minimal utility in normal pts

D&T 2: Exam 2 (5 decks)

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