Druhgs Flashcards
(101 cards)
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
2
Q
Hydromorphone
A
Derivative compound of morphine that is used for VERY SEVERE pain
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
4
Q
What is the urinary metabolite of heroin?
A
6-monoacetylmorphine
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
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
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
8
Q
Buprenorphine
A
Partial u-agonist/k-antagonist; approved for the treatment of opioid dependence
***Used for pregnant drug addicts
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
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
11
Q
Clonidine
A
Alpha-2 adrenergic that inhibits pain in the dorsal horn projection neurons
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
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
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
15
Q
Metaxalone
A
Uses: Muscle Discomfort
ADR: Jaundice, CNS depression, do not use w/ renal impairment
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)
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
18
Q
Tissue Kallikrein System
A
Tissue Kallikrein converts LMWKG to kallidin
Kallidin is then converted to bradykinin via aminopeptidase
19
Q
Kininase I
A
Carboxypeptidase N and M; cleaves kinins into ACTIVE metabolites
20
Q
Kininase II
A
ACE; converts bradykinin into an INACTIVE metabolite
21
Q
B1 Kinin Receptor
A
Activated by Bradykinin and its metabolites; expression is induced by inflammation
22
Q
B2 Kinin Receptor
A
Activated by native Bradykinin and kallidin; constitutively expressed
23
Q
CGRP
A
Calcitonin Gene Related Peptide; most potent vasodilator of the trigeminal system
-Excess release causes migraine
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
25
5-HT receptors (1D and 1B)
1D =>>induces vasoconstriction of cranial blood vessels
1B =>> Inhibits nociceptive trigeminal afferents; big role-player in migraine tx
26
Prophylactic Tx of Migraines and side effects
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
27
Abortive Migraine Drugs
Mild: NSAIDs
Moderate: Ketorolac; only use for 5 days or else will cause GI damage
Children: No aspirin
Preggers: NSAIDs ok until 3rd trimester
28
Ergot Alkaloid Mechanism and Side Effects
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
29
Triptan mechanism
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)
30
Sumatriptan
Short onset and duration of action; very short plasma t^1/2
-Relief only for about 2 hrs
31
Naratriptan and Zolmitriptan
Given orally and has better bioavailability and longer duration of action than sumatriptan
-Lower dose for renally impaired pts.
32
Flovatriptan
Longest acting triptan w/ highest affinity for 5-HT1B receptor BUT has long onset of action
33
Rizatriptan (sounds like eliza)
Quick dissolving sublingual tablet w/ a faster onset of action and les N/V than sumatriptan
34
Timeline of neuroleptic therapy
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
35
Haloperidol
Typical neuroleptic drug that is also used to treat Huntington's Tourette's
36
Chlorpromazine
Phenothiazine typical neuroleptic that is used for hiccough but is contraindicated in pts. w/ seizures
37
Thioridazine
Typical neuroleptic that deposits in the retina at high conc.
***Cannot be used as an anti-emetic as well as aripiprazole
38
Extrapyramidal side effects of neuroleptics
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
39
Tardive Dyskinesia
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
40
Neuroleptic Malignant Syndrome
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
41
Prolactin and Neuroleptics
Excessive secretion can occur due to blockade in the tuberoinfundibular pathway; most common w/ phenothiazines
-Produces issues w/ compliance
42
Cholinergic effects of neuroleptics
Dry mouth, blurred vision, urinary retention, constipation
-Thioridazine, Chlorpromazine, Olanzapine, Clozapine (no dry mouth tho)
43
Metabolic Side effects of neuroleptics
Most common w/ atypicals (especially clozapine, olanzapine) but also significant w/ chlorpromazine
-Potential leukopenia w/ clozapine
Risperidone =>> slight weight gain
Haloperidol =>> possibly nothing
44
Rabbit Syndrome
Perioral tremor assoc. w/ longterm use of neuroleptics
-Tx w/ anticholinergic antiparkinson drugs
45
Contraindications to Neuroleptics
***Pregnancy
-Amphetamine use, anticholinergics (worsens extrapyramidal sx), SSRIs, antihypertensives
46
Opiod Abuse
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
Benzodiazepine abuse
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
Propofol
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
Amphetamine Abuse
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
MDMA
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
Cocaine Abuse
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
Cocaethylene
Cocaine and alcohol metabolic byproduct capable of crossing the BBB and being just as potent as cocaine
53
Levamisole
Used to cut cocaine and induce stronger effects; can cause agranulocytosis and neutropenia
54
Bath Salts
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
Nicotine
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
Caffeine (Methyxanthine)
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
Lysergic Acid Diethylamide
5HT-1 agonist that serves as a hallucinogen w/ brilliant colors and mood elevation; haloperidol can block hallucinations
58
Mushrooms
Utilizes psilobycin to produce hallucinations but causes mydriasis, confusion, vertigo, N/V
-Tx w/ diazepam
59
Ketamine
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
Anesthesia stages
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
Localized Anesthetics
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
Vasoconstrictor effect on anesthetics
Prolongs the effect of anesthetics by slowing the absorption and decreasing the amnt of side effects
63
Topical anesthetic for skin
Benzocaine
64
Bupivacaine
Injected into the epidural space of pts. in labor and it is then absorbed into systemic circulation
-Prevent cardiac depression and CNS toxicity
65
Autonomic Nervous System of the Eye
a1 receptors =>> iris dilator, Mueller muscle
B2 =>> Ciliary muscle
Muscarinic =>> Iris sphincter, ciliary muscle
66
Phenylephrine
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
Aproclonidine
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
Brimonidine
***GO-TO for NTG; highly selective for a2 receptors
69
Cocaine Opthalmological Use
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
Hydroxyamphetamine
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
Dapiprazole
Reverses mydriasis; competitively binds to postsynaptic receptors of the iris dilator muscle
72
Timolol
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
Betaxolol
B1 selective blocker that is less potent than Timolol but is ok to used in COPD pts.
74
Carteolol
B-blocker w/ intrinsic sympathomimetic activity; competes for B-adrenergic receptors and only has limited activity when it does bind
-No selectivity
75
Pilocarpine
***Used to treat acute angle closure glaucoma
-Works by inducing miosis and activating the constrictor muscle
76
Carbachol
Causes longer lasting miosis than pilocarpine and can be used in cataract surgeries
77
Homatropine
Cholinergic antagonist that Produces great mydriasis and cycloplegia
***Used to reduce pain in uveitis
78
Atropine
Cholinergic antagonist that has THE BEST mydriasis and cycloplegia
***Used in eye exams for children BUT CANT USE IN DOWN SYNDROME PATIENTS
79
Cyclopentoate
Cholinomimetic drug that is used as a mydriatic in pediatric ocular examination
80
Neurology of ADHD
Impusilveness/Hyperactivity- Alterations within the orbitofrontal complex
Inattentiveness- Alterations in the dorsolateral prefrontal cortex and the dorsal anterior cingulate cortex
81
Treatment of ADHD
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
Treatment of Oppositional Defiance Disorder and Conduct Disorder
ADHD Medications- (Ritalin, Amphetamines, Clonidine)
Mood stabilizers- Lithium, VA
Anti-psychotics- Risperidone, apripazole
83
Treatment of Autism Spectrum Disorders
Inattention and Hyperactivity- ADHD, anxiety drugs (SSRIs, risperidone)
Disruptive behavior- Risperidone, SSRIs, atypical neuroleptics, clonidine
Repetitive Behavior- Fluoxetine, Risperidone
84
Tourette's Neurology
Likely due to disinhibition of the cortico-striatal-thalamic cortical loop causing increased activity of the caudate nucleus
85
Treatment of Tourette's
Tics- Atypical antipsychotics (D2 agonists, Fluphenzaine, Pimozide), Tetrabenazine, Botox
Behavioral sx- Clonidine, SSRIs
86
Status epilepticus
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
Phenytoin (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
Carbamazepine (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
Phenobarbitals (in epilepsy)
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
Valproic Acid (B)
VALPO-FLAKES
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
Ethosuximide
Mech: Blocks t-type Ca2+ channels of thalamic interneurons
Uses: ABSENCE SEIZURES (guess what pathways are interrupted in them)
92
Lorazepam, Diazepam, Clonazepam (antiepileptics)
Mech: Bind to GABAa receptor promoting its fnxn
| =>>Abrupt withdrawals can cause rebound seizures
93
Lamotrigine (A,C)
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
Topiramate (antiepileptic)
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
Levetiracetam
Used as an adjunct usually but is good for pts. w/ bad livers; will help the liver metabolize potentially damaging drugs
96
Oxcarbazepine
Mech: Blocks voltage-gated Na+ channels
Uses: Partial seizures, medication resistant epilepsy
ADRs: Hyponatremia for the first 3 months
97
Fetal Hydantoin Syndrome
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
Prochlorperazine
Typical antipsychotic given during chemo because it is an effective anti-emetic
99
When can you consider opioid detoxification for a pregnant patient?
If pt. Is taking less than 40mg a day and the fetus is less than 20 weeks old
100
Longest lasting pain reliever on the market
OxyContin
-Hillbilly heroin
101
What drug is safe to use to produce Mydriasis and cycloplegia in glaucoma patients?
Tropicamide- a Cholinergic antagonist with minimal utility in normal pts
