Neurology and Psychiatric Drugs Flashcards
1
Q
Name the centrally acting skeletal muscle relaxants
A
Diazepam (Benzodiazepene)
Tizanidine (α2 agonist)
Baclofen
2
Q
Diazepam
A
-Benzodiazepine (“long tapering flag”)
- increase frequency of oppening of the chloride ion channel
- binds at allosteric site on GABA-A receptor which is a chloride channel and potentiates GABA effects →Cl- influx →hyperpolarization→less neuronal excitation
- indicated for spasticity induced by neurological disorders (e.g. MS)
- produces sedation at required dose for reduction of muscle tone
- can induce withdrawl affects
3
Q
Tizanidine
A
-α2 agonist
- inhibits release of excitatory Amino acids thus re-inforcing both pre/postsynaptic inhibition in the spinal cord
- indicated for spasticity induced by neurological disorders (e.g. MS)
- produces sedation at required dose for reduction of muscle tone
- can induce withdrawl affects
5
Q
Dantrolene
A
- block RYR1 receptor → decreasing free intracellular calcium concentration.
- treats malignant hyperthermia which is a condition resulting from defective RYR receptors in the Sarcoplasmic reticulum
- useful for spinal injuries ,spasm after stroke
- may cause severe liver toxicity
6
Q
Botulinum toxin
A
- exotoxin of clostridium botulinium
- controls release of Ach from vesicles by binding to synaptobrevin
- treats ophthalmic / local muscle spasms
- local facial injection are used for treatment of wrinkles
- present on honey - shouldn’t be given to children < 1 y.o.
- may cause flaccid paralysis
8
Q
Baclofen
A
- GABA-B agonist
- GABA-B receptor is a K+ channel →increase K+ influx →hyperpolarization →Ca+2 ion influx decrease → decrease release of excitatory NTs
- rapid ,complete absorbtion after oral adminstration
- used for spasticity induced by neurological disorder (e.g. MS)
- less sedative but also less effective than Diazepam
- enhances sedative/resp dep. effects of opiates
9
Q
Non depolarizing muscular relaxant
A
- competitive antagonists preventing Ach to depolarize the muscle cells
- at higher doses they produce more intense motor blockade
1st -muscles of face,eyes
2nd -finger,limbs neck trunk
3rd-intercoastals , diaphragm
- useful for anesthesia and facilitation of intubation
- can be reversed by **Neostigmine
Isoquinolone dervatives -**
- Tubocurarine
- Atra-curium
- Cistra-curium
Steroid dervatives -can be reversed by Neostigmine
-Pan-curonium
-Ro-curonium
*have vagolytic effect +enhance NE release
10
Q
Depolarizing muscle relaxant
A
- depolarize muscle cells similarly to Ach however they are more resistant to degradation by AChE therefore n-AChR is incapable of transmitting further impulses because of the resistance to depolarization
- can lead to flaccid paralysis
- During phase I the reaction is irreversible
- useful for rapid endotracheal intubation or during electroconvulsive shock
11
Q
how are benzodiazepens classified ?
name Benzodiazepens for each category
(“Ben’s Diner”)
A
-have “PAM-suffix
(“Pam-cakes in Ben’s diner”)
-have “OLAM-suffix”
(“pamcakes offered ALL A.M.”)
——————————————————————————–
Short acting Benzodiazepens -“ATOM”
Triaz-olam
Oxaze-pam (“fast ox”)
Midaz-olam
——————————————————————————–
Intermediate acting Benzodiazpenes “lora the clown”
Loraze-pam
Alpraz-olam
Clonaze-pam
——————————————————————————–
Long acting Benzodiazpenes
Diaze-pam
Fluraze-pam
12
Q
Benzodiazpenes MOA
(“Ben’s Diner”)
A
-bind to an allosteric site on GABA-A Receptor
(“Ben’s diner coworker handing the Cab-A driver Pamcakes”)
-GABA-A receptor is a chloride channel, chloride influx hyperpolarizes nerve cells
(“chlo-rider” sign on Cab-A)
-Benzodiazpenes increase the Frequency of opening of the chloride channel
(ben’s diner is :”now open more frequently”)
-potentiates (enhance) transmission of GABA in CNS
(“Red CNS light on Cab-A”)
-GABA is the major inhibitory neurotransmitter in the CNS (the sign on Cab-A says “take it easy” )
-metabolized by the liver and produce long acting active metabolites
(“fast ox has liver spot on him”)
-have addictive potential
(“Ben’s Diner pamcakes have addictive flavour”)
13
Q
what are Benzodiazepens used for ?
(“Ben’s Diner”)
A
-IV adminstration of Benzodizapenes are useful in managment of alcohol withdrawl , seizures , anesthesia (“Ivy on pole”)
-IV adminstration of Benzos can be used for general anesthesia
(“green shirt sedated customer with straw in mouth”)
-IV adminstration of Benzos is useful to induce
conscious sedation for minor procedures ,e.g.-colonoscopy
(cup saying “lite” infront of sedated customer)
——————————————————————————–
-useful for treatment of status epilepticus
(“coworker unplugging jackhammer”)
- can treat insomnia (“customer sleeping on table”)
- **not 1st line due to physical dependence**
-can treat Parasomnias in children
(“crying kid in pajamas”)
-benzos are muscle relaxants used to treat Spasticity cause by upper motor neuron disorders
(“red shirt blacky relaxed on diner’s bench”)
- useful in treatment of General Anxiety Disorder {G.A.D}
- *SSRIs/SNRIs are 1st line
(“Anxious cutsomer not sure if he can pay for the date lool”)
- Benzos are useful for treating Panic disorder
- *SSRIs/SNRIs are 1st line
14
Q
Benzodiazepens side effects
A
-can potentially cause addiction
(pam-cakes have “addictive flavour”)
-can cause tolerance (“all are welcome” sign in Ben’s Diner)
-Benzodiazepens can cause Anterograde Amnesia and learning impairment
(“question mark hat on sedated customers head”)
- useful for conscious sedation so patient will follow orders but will forget unpleasant procedure afterwards
- Benzos can cause Central Ataxia causing elderly patient to fall
(“unbalanced stack of pamcakes infront of old fart”)
-elderly patients are more sensitive for Benzos side effects (“disoriented man sitting infront of stack of unbalanced pamcakes”)
- adminstration of Benzos should be avoided with other CNS depressants such as 1st generation antihistamines
(“coworker with bee swatter smacks old fart customer”)
16
Q
what are the alcohol withdrawal symptoms
? what role do Benzos have in treating alcohol withdrawal
A
-alcohol also binds GABA-A receptor but on a different allosteric site
(“alcoholic guy is on back of Cab-A”)
-Benzos are useful in treatment of alcohol withrdawl symptoms (“hangover special pamcakes”)
- especially long acting Benzos such as Diazepam and Chlordiazepoxide
(“Long tapering flag on hangover special pamcakes”) - for patients with hepatic insufficiency use short-acting Benzos
Alcohol Withdrawal symptoms -“3 alcohol specialists”
1st specialist (8-12 hours) - insomnia ,tremulousness , anxiety , autonomic instability
2nd specialist (12-48 hours) - Seizures
_3rd specialist (_48-96 hours)-**delirium tremens** (fever ,disorientation , severe agitation )
17
Q
what is the key difference between Benzodiazepens and Barbiturates
A
-the difference between them is that Barbiturates bind different allosteric site on GABA-A receptors
(“barber shop located on other side of Cab-A”)
18
Q
How can you reverse Benzodiazepens-induced sedation
A
-Flumazenil is a competitive antagonist at the BZD receptor and can reverse Benzos-induced sedation
(“violent-antagonizing fluffy muzzled dog”)
19
Q
Name the non-Benzodiazepine hypnotics
(“catching some Z’s”)
A
the 3 Z’s
Zolpidem
Zaleplon
esZopiclone
20
Q
non-Benzodiazepine hypnotics MOA
A
-bind same allosteric site as Benzodiazepines at GABA-A receptor
(“ben’s diner coworker and zzz mattresses coworker are grabbing the same Cab-A handle”)
-GABA-A receptor is a chloride channel,chloride influx hyperpolarizesnerve cells
(“chlo-rider” sign on Cab-A)
-potentiates (enhance) transmission of GABA in CNS
(“Red CNS light on Cab-A”)
-GABA is the major inhibitory neurotransmitter in the CNS (the sign on Cab-A says “take it easy” )
-Barbiturates bind different allosteric site on GABA-A receptors
(“barber shop located on other side of Cab-A”)
-alcohol also binds GABA-A receptor but on a different allosteric site
(“alcoholic guy is on back of Cab-A”)
21
Q
Pharmakokinetics of Zolpidem Zaleplon es-Zopiclone
A
-Zolpidem and Zaleplon are fast acting non-Benzos with rapid onset (sheeps sign says :”fall asleep FAST”)
-Non-benzos hypnotics have short duration of action
(“sheeps quick jump and fall on sign”)
-Zolpidem and Zaleplon are metabolised by the liver
(“sheeps on sign have liver spot on them”)
23
Q
Side effects on non-Benzos
A
-elderly are more sensitive to the side effects
-can cause Central Ataxia
(“unbalanced stack of pillows”)
-avoid use with other CNS depressants
(“cannot combine with other CoupoNS”)
- e.g.- 1st Gen. Antihistamines
(“bee swatter coworker hitting old fart”)
24
Q
what are non-Benzodiazepene hypnotics used for ?
A
-useful in treatment of insomnia
- Zolpidem and Zaleplon are short-acting and therefore useful in treating Sleeep onset insomnia and not for maintaining sleep
- esZopiclone has longest half life and is therefore effective for both falling asleep and maintaining sleep
-less likely to cause withdrawal symptoms
(“sale sign says break those bad sleeping habits”)
-non-benzos are less likely to cause tolerance
(sale sign says “returns not tolerated”)
26
Q
how can you reverse non-benzos sedation ?
A
Flumazenil - BZD Competitive antagonist
(“fluffy muzzled dog biting on zzz matresses red arrow sign”)
27
Q
what other drugs can be used to treat insomnia ? MOA?
(“let your sleepless nights melt away”)
A
- *Melatonin**
- *Ramelteon/Agomelatin** (melatonin receptor agonists)
-MT1 and MT2 melatonin receptors are found in the suprachiasmatic nucleus of the hypothalamus and are activated by Ramelteon
(“nucleus above x shaped ceiling fan”)
- **-Ramelteon has no direct effects on GABA-ergic transmission in the CNS **
- melatonin receptors maintain the Circadian rythm (“light and dark spotlights”)
-Ramelteon/Melatonin have fewer side effects and are safer in Geriatric patients
(peacefully sleeping old fart below “melt-away sign”)
28
Q
Name Barbiturates
A
Thiopental
(“The Ol’ quick shave”)
Primidone
(“Perm is done!” primadona)
Phenobarbital
29
Q
Barbiturates MOA
A
-GABA-A receptor is a chloride channel,chloride influx hyperpolarizes nerve cells
(“chlo-rider” sign on Cab-A)
-potentiates (enhance) transmission of GABA in CNS
(“Red CNS light on Cab-A”)
-GABA is the major inhibitory neurotransmitter in the CNS (the sign on Cab-A says “take it easy” )
-binds to a separate allosteric site on GABA-A Receptor
(“barber opening dooe on other side of Cab-A driver Pamcakes”)
-Barbiturates increase the duration of opening of the GABA-A receptor chloride channel
(sign at entrance of shop saying :”long hair? now open longer”)
-Barbiturates have long duration of action and therefore “hangover” effects are more common
(“long tapering flag outside barber shop”)
30
Barbiturates **Pharmacokinetics**
| (mainly Thiopental here?)
-**Barbiturates** have **long duration of action** and therefore "hangover" effects are more common
("long tapering flag outside barber shop")
- Thiopental has **rapid onset** and **short duration** of action because it's _highly lipid soluble_
- plasma levels of **_Thiopental_ decrease rapidly** due to **redistribution** to **skeletal muscle** and **adipose**
("barber cuts hair and redistributes it to arms and belly of customer")
_Redistribution graphof Thiopental (on customer's chest_)
**Decay line** - rapid decay of _plasma_ Thiopental
**Brief peak -** rapid accumulation of thiopental in _brain_ and rapid redistribution
**Growth line**-rapid accumulation of Thiopental in _skeletal muscle_ and _adipose_(recovery from anesthesia)
32
Barbiturates **side effects**
-chronic use of barbiturates leads to **tolerance**
("all are welcome" sign in entrance of barbershop)
-chronic barbiturates use leads to **physical dependence**
("addicted to curls" sign)
-can cause **hypotension**
("fainted old fart sitting on hair dryer chair")
-can cause profound **cardiac and respiratory depression**
("old fart has collapsed heart and lungs t-shirt")
-can cause **severe CNS depression** (coma) ,should be avoided in elderly
("brain shaped hair dryer")
**-**barbiturates are **potent inducers** of the **CYP450** which may **increase metabolism** of drugs such as **warfarin**
(activated chrome bumper plate saying "CYP450")
33
what are **Barbiturates used for ?**
**_IV-adminstration of Barbiturates_** _("Ivy on pole")_
**-IV adminstration** of **_Thiopental_** can be used for **induction of anestehsia** since its highly lipid soluble and enters the CNS quickly.
(intubated customer getting "The Ol' quick shave")
-**IV adminstration** of **_Phenobarbital_** can be used to treat **Seizures**
("coworker outside unplugging jackhammer")
-**_Primidone_** ("perm is done!") can be used to treat **seizures** and **essential tremors -** 1st line with propanolol
("prima dona's barber has tremulous hand")
35
name the **IV Anesthetics**
| ("Ivy on all damn poles")
**Propofol**
(Introducing Prospero "fall asleep" the hypnotist)
**Etomidate**
(Introducing the beast from the east "THE INTIMIDATOR")
**Ketamine**
(Introducing "snaKE TAMINg" _nomad_ )
**Benzodiazepines**
("Ben's Diner")
**Thiopental**
("The ol' quick shave")
36
**Propofol**
| (prospero "fall asleep" the hypnotist)
-**potentiate** **chloride** current through the **GABA-A** receptor complex
("old Cab-A behind prospero's stand")
-can be used for **induction** of anesthesia
(introducing prospero "fall asleep" the hypnotist)
-can be used for **maintenance** of anesthesia
(sign next to prospero says :"try to MAINTAIN your sanity!")
-propofol cause **profound vasodilation** (arterial+venous)
37
**Etomidate**
| ("introducing the beast from the east the INTIMIDATOR")
-potentiates **chloride current** through the **GABA-A** receptor complex
("old Cab-A behind the INTIMIDATOR stand")
-is an IV anesthetic for **induction**
("_introducing_ the intimidator")
-Etomidate preserves **cardiovascular stability**
("the buffy intimidator stabilizes the patient ")
38
**Ketamine**
("snaKE TAMINg)
-**inhibits** the **NMDA recepto**r complex which is a glutamate receptor and ion channel
("hitched nomadic camel")
-can be used for **induction** of anesthesia
("introducing the snaKE TAMINg nomad")
-causes **"dissociative anesthesia"**
("man looking in snakes eye causing dissociative trance")
-can cause unpleasant **emergence reactions**
* vivid colorful dreams
("colorful steam from snakes bucket")
* hallucinations
* out of body experiences
-can cause **cardiovascular stimulation{Incr.BP HR CO}**
("stimulated cobra's head shaped like heart")
42
**Benzodiazepines**
("Ben's Diner")
Midaz-olam ,
Loraze-pam
-IV anestheic used **preoperatively**
-used for **conscious sedation** for **minor procedures** such as **colonoscopy**
("bowel water pump outside Ben's Diner")
43
**Barbiturates**
("Barber's shop)
**-Thiopental** has **rapid onset** and **short duration** of action since it is **highly lipid soluble**
("The Ol' quick shave")
-IV Anesthetic used for **induction** of anesthesia
("_Introducing_ the BARBER SWEENY PENTAL")
44
**Neurolept Analgesia**
**_Neuroleptanalgesia_**
- a state of **analgesia ,sedation, muscle relaxation** BUT no loss of consciousness
- **Fentanyl + Droperidol**
- contraindicated in **parkinsonism**
- useful during diagnositc procedures requiring cooperation of the patient
**_Neuroleptanesthesia_**
- Fentanyl+Dorperidol, **Nitrous oxide**
- addition of NO **improves amnesia**
45
**Peri-operative** medications
_Before surgery_
-IV. Barbiturates - **Thiopental** ("the ol' quick shave")
-Sedative/Anxiolytic Benzodiazepine -**Diazepam** ("long tapering flag")
-Antimuscarinic - parasympatholytic agent -**Atropine("alice")**
-Analgetics - **Opiods** (fentanyl) non opioids
---------------------------------------------------------------------------------------------------
_During surgery_
-NMB- **Succinylcholine** (depolarizing) / **Curare derivatives** ( non-depolarizing)
-Pressors in case of shock - **Norepinephrine**
---------------------------------------------------------------------------------------------------
_After surgery_
-If opioids were used before surgery - **non-opioids** should be used
-antagonism of NMB -**Neostigmine**
-antagonism for opioids if respiration is too slow - **Naloxone**
46
Gaseous anesthetic
Nitrous Oxide (N2O)
47
Volatile anesthetics
Enflurane
Isoflurane
Halothane
48
Volatile anesthetics pharmacodynamics
-volatile anesthetics are **liquid at room temperature**
(e.g. enflurane, isoflurane, halothane)
("Air tank in water")
-volatile anesthetics are **fluorinated**
(e.g. enflurane, isoflurane,halothane)
("Balloon flower")
**-highly soluble** inhaled anesthetic (e.g. halothane)
("Moving freely in ball pit")
**more soluble** inhaled anesthetics (e.g. halothane) have a **slower onset of action**
("Passed out later")
-**more soluble** inhaled anesthetics (e.g. halothane) have a **longer duration of action** ("Long tapering flag")
- Partition\>\>\>: higher blood:gas partition coefficient
(e. g. halothane) → higher solubility → **slower onset of action
- ---------------------------------------------------------------------------------**
Less steep arterial tension curve (e.g. halothane) → higher blood:gas partition coefficient→higher solubility → **slower onset of action**
49
Nitrous Oxide Pharmacodynamics
**less soluble** inhaled anesthetic
("Impeded by ball pit")
(e.g. N2O)
less soluble inhaled anesthetics (e.g. N2O) have a **faster onset of action**
("Passed out earlier")
less soluble inhaled anesthetics (e.g. N2O) have a **faster recovery**
("Immediate rescue" )
Steeper arterial tension curve (e.g. N2O)→ lower blood:gas partition coefficient→ **lower solubility → faster onset of action**
50
Volatile Anesthetics side effects
-inhaled anesthetics can cause **respiratory depression** (leading to decreased minute ventilation and hypercapni a)
("Deflating lung balloons")
-**myocardial depression** →hypotension
("deflating heart balloon")
-fluorinated anesthetics **increase cerebral blood flow** (decrease cerebral vascular resistance)("Red brain wig")
halothane can be **hepatotoxic**
(e.g. massive hepatic necrosis) ("Cracked liver")
enflurance can be **nephrotoxic** ("Smacked in the flank")
enflurance can induce **seizures** ("Shaking")
**-malignant hyperthermia**
(skeletal muscle hypersensitivity to volatile anesthetics) ("Magnificent birthday")
51
MAC
_minimum alveolar concentration (MAC)_
**MAC** corresponds to the **dose** of anesthetic that causes **50%** of patients to become **unresponsive to painful** stimuli
("1 out of 2 unresponsive")
**1/MAC** corresponds to the **potency** of an inhaled anesthetic ("Inverted bowl of potent mac and cheese")
53
what is the **treatment** of malignant hyperthermia
**Dantrolene
-----------------------------------------------------------------------------------**
Blocking Ryan: dantrolene **blocks ryanodine receptors**
-treats malignant hyperthermia
57
**malignant hyperthermia**
-**succinylcholine** (depolarizing muscle relaxant) can also causes **malignant hyperthermia**
malignant hyperthermia is related to a **defect in ryanodine receptors** (RyR) in the sarcoplasmic reticulum
-excess **heat production** and consumption of ATP induces **rhabdomyolysis**
58
what is the **mechanism of action** of SSRIs ?
-**inhibit presynaptic reuptake** of Serotonin
("worker in sitcom keeps post-it stick notes out of the drawer")
59
name the **SSRIs**
("travel posters behind expre**SS tR**Ips")
_Selective Serotonin Re-uptake Inhibitors_
**Paroxetine**
("Parrot air" poster)
**Fluoxetine**
("Fly out"poster)
**Sertraline**
("Desert Airline" poster)
**Citalopram**
("the City" poster)
60
MOA of **SNRIs**
-inhibit **presynaptic re-uptake** of **Norepinephrine** and **Serotonin**
("North and South compass poster above dual copy machine ")
61
Name the **SNRIs**
_SNRIs_
**-Venlafaxine**
("_fax_ machine infront of compass poster")
-**Duloxetine**
("**_Dua_**l copy machine below compass poster")
62
what can SSRIs **_AND_** SNRIs be used for ?
- **1st line** treatment for **depression {M.D.D}**
* \*slower onset than Benzos so not useful for treatment of acute symptoms \*
-**1st line** treatment of **G.A.D**
(Anxious coworker holding "preformance repot")
-useful for treatment of **panic disorder**
("the scream saver")
-useful for treatment of **PTSD**
(coworker holding dog tags saying "PT" and SD")
| ("happy/sad masks logo on right edge of sitcom")
63
what can **SSRIs specifically** be used for?
-useful in managment of **OCD**
("obsessively neat coworker re-arranging his table")
**-**
useful in treatment of **Bulimia**
(blonde coworker opening "binge snack drawer")
-useful in treatment of **Social Anxiety Disorder**
("shy coworker hiding behind desk ")
64
what can **SNRIs specifically** be used for?
-useful for treatment of **Diabetic Neuropathy**
("coworker feeling pain from Diasweeties machine")
-useful in treatment of **chronic pain (neuropathic)**
("chronically frayed wires from diasweeties machine")
-useful in treatment of **fibromyalgia**
("fiber bars at top shelf in diasweeties machine" )
65
how long should you wait before considering an alternative treatment for SSRIs/SNRIs ?
-SSRIs and SNRIs take **1-2 months** to achieve maximum effect
| ("2 months calendar behind shy guy")
66
what are the **Side effects** of SSRIs ?
-hyponatremia as a result of **SIADH {incr. ADH}**
("inappropriately wet head of blacky coworker")
-SSRIs can cause **Sexual Dysfunction**
("patty rejects and throws paper clips in ugly guy's face")
-SSRIs can cause **weight gain**
("fat guy next to expreSS tRIps counter")
-SSRIs can cause **Drowsiness**
("purple shirt coworker sleeping on the job")
67
what condition may percipitate as a result of SSRIs and SNRIs abuse ? what are the characterisitc findings of this condition ?
-SSRIs and SNRIs may cause **Serotonin Syndrome**
("excessive smiley post-it sticky notes in back office")
-**combination** of SSRIs/SNRIs with other drugs may also cause **serotonin syndrome** {e.g. TCAs,MAOis}
("Tricycle and mouse traps in smiley backoffice")
-serotonin syndrome is characterized by **hyperthermia** and **hypertension**
("michelle boss of the office is hot and has steam coming out of his ears")
-characterized by **neuromuscular hyperactivity , hyperreflexia , clonus**
("boss of office hyperactive foot tap")
68
what is the **treatment** for Serotonin Syndrome ?
**Cyproheptadine** (5-HT2 blocker)
(boss of the office holding sign saying "silly pranks prohibited")
69
what are the **side effects of SNRIs**?
-SNRIs can cause **hypertension**
("hypertensive coworker has steam coming out of his ears because of the fax machine")
70
what are the withdrawl symptoms observed after stopping adminstration of SSRIs/SNRIs ?
- withdrawl symptoms from SSRIs/SNRIs include **Flu-like symptoms**
| (office phone has sticky note saying "out with the flu")
71
Name the **tertiary** Tricyclic Antidepressants
**Imipramine**
("**_Impr_**int on green shirt boy's face")
**Amitriptyline**
("green shirt boy **_trip_**ping from tricycle")
_secondary amines_
**Nortriptyline
Desipramine**
72
Name the **Secondary amine TCAs**
_"**NOR**th si**DE** prep secondary school"_
**Nortriptyline**
**Desipramine
-**
secondary amines have **less anticholinergic effects** (woman protected by "Northside prep" sign
\*most appropiate for the elderly\*\*
73
what is the **MOA** of TCAs ?
TCAs **inhibit presynatpic uptake** of **serotonin** and **norepinephrine** NET/SERT
("green shirt boy prevented from picking up smiley and compass balls")
74
what can TCAs be used for ?
-useful in treatment of **resistant depression**
("happy/sad mask next to resistant door that kid can't open")
-useful in **diabetic neuropathy**
("kid having pain from diasweeties machine")
-useful in treatment of **chronic pain (neuropathic)**
("chronically frayed wire next to diasweeties machine")
-may be used for **migraine prophylaxis**
("pounding headbell" )
* \*\*Amitriptyline is the only TCA with proven efficacy\*\*
-Clomipramine(secondary amine) can treat **OCD**
("obessively neat kid re-arranging his marbles")
* \*\*not as 1st line treatment - SSRIs are.\*\*
75
what are the **side effects** of TCAs?
-TCAs can cause **Sexual dysfunction**
("gym teacher rejected by Mrs. Pearson")
-can cause **Seizures**
("ball hits yellow shirt kid and he becomes shakey")
--------------------------------------------------------------------------------
-TCAs (mostly tertiary) have severe **antimuscarinic effects i**ncluding:
* dry mouth ("dry as a cracker")
* constipation
* blurred vision ("blind as a bat")
* urinary retention ("full bladder shaped tea kettle")
* CNS effects ("mad as a hatter")
\*\*the antimuscarinic effects are the most common side effects among all TCAs side effects \*\*
\*\*\*the most potent antimuscarinic effects are exerted by Amitriptyline\*\*\*
\*\*\*\*TCAs are **contraindicated** in **elderly** because of these severe antimuscarinic/antihistamine effects\*\*\*\*
- -------------------------------------------------------------------------------
- TCAs **block H1 receptors** ("blacky with bee swatter")
* leads to **sedation**
("blue shirt kid sleeping on table")
leads to increased appetite **weight gain**
("red shit fat kid next to sleeping kid")
--------------------------------------------------------------------------------
-TCAs **block α1 receptors**
("pink shirt girl holding single extinguished candle")
* may cause **orthostatic hypotension**
("pink shirt girl next to tea party is passed out")
--------------------------------------------------------------------------------
-TCAs can cause **Serotonin syndrome**
("stack of smiley balls behind blue shirt dodger")
76
what are **cardiac side effects** cause by TCAs ? what is the treatment for these undesired effects ?
-TCAs block cardiac **fast Na+ channels** that may cause fatal cardiac arrhythmias
("inactivated peaNa+ butter jar")
-can cause **wide QRS complex** on ECG
("Wide QRS-shaped crack in heart sign")
-can induce **Torsades de pointes** ventricular tachycardia
("twisted Torsades streamer")
\*\*the most common cause of death of patients treated with TCAs is TCA overdose causing fatal cardiac arrhythmias
("dodge ball hitting peaNa+ butter cookie stand and breaking \<3 cookies"
- -------------------------------------------------------------------------------
- **Sodium Bicarbonate** can be used to treat widened QRS and ventricular arrhythmia caused by TCAs overdose (white
77
name the **MAO enzymes** and their actions !
**-MAO-A** ("albino mouse") breaks down **Serotonin** , **Norepinephrine** , **Dopamine**
("white mouse eating smiley cheese , compass cheese and dopa rope")
**-MAO B** (" black mouse") breaks down **dopamine exclusively** ("black mouse eating rope")
78
name **non-selective MAOis**
**Tranylcypromine**
("Try a sip of wine !" sign on table)
**Phenelzine**
("Funnel in wine bottle on table")
**Isocarboxazid**
("Boxed wine on table")
79
what are **MAOis used for**?
-MAOis are **irreversible**
("mouse skeleton trapped in mouse trap)
-useful in treatment of **Atypical depression**
("Chateu Tyramine ...not your typical winery")
-useful in treatment of **depression** (not 1st line)
("happy/sad mask on chateu tyramine sign")
-useful in treatment of **resistant depression**
("guy trying to open resistant wine bottle with happy/sad mask label")
80
-name **selective MAOis inhibitor**
**Selegiline -** selective MAO B inhibitor
("guy on ladder with _sledge hammer_ trying to hit black mouse")
**Moclobemide** - selective MAO A inhibitor
81
what are **selective MAOis used** for ?
-useful for treatment of **Cogwheel rigidity** seen in **Parkinson's disease** since they **increase Dopamine** levels in the **CNS**
| ("watch runing by cogwheels above sledge hammer")
82
what are the **side effects of MAOis ?**
-since non selective MAOis inhibit serotonin breakdown they have **similar side effects to SSRIs** including:
* highest rate of **sexual dysfunction** among anti depressant
* **orthostatic hypotension**
* **weight gain**
-**should be avoided** with tyramine containing foods such as **aged meats , wine and cheese**
("wine and cheese on table")
-**tyramine** is usually **broken down** in the GI by **MAO enzymes**
("albino mouse eating GI meat")
**-**when MAOis are adminestered tyramine is **not broken down** and **act as sympathomimetic**
("albino trapped in mouse trap and NE compass cheese released")
-**Tyramine Toxicity** can percipitate a **hypertensive
crisis**
("blonde lady is hypertensive and sweaty having steam come out of her ears ")
-may cause **Serotonin Syndrome**
("pile of smiley cheese next to tricycle")
-**should be avoided** with other drugs such as **TCAs** and **SSRIs**
("yellow tricycle in front")
83
what drug could be adminesterd for **management of hypertensive crisis** resulting from Tyramine toxicity ?
**Phentolamine**-reversible α1 and α2 antagonist ("phantom of the alpha behind blonde lady")
84
Name **Atypical Antidepressants**
**Bupropion (Unicyclic)**
("blacky pro ball player")
**Mirtazapine (Tetracyclic)**
("mirth and misery" happy/sad mask)
**Trazodone**
("cheerleader with Trombone")
85
Bupropion **MOA**
**Inhibits reuptake** of **Norepinephrine** and **Dopamine** via NET/DAT ("NET DAT ball pro")
\*\*no effects on serotonin !- no smiley symbols\*\*
86
what can **Bupropion be used for ?**
-atypical antidepressant that used for treatment of **depression** associated with **hypersomnolance** (daytime sleepness) since it has **CNS activating effects** via **NE**
("depressed blue shirt boy aroused from sleep") \
-can be used for treatment of **tobbaco dependence**
("pros don't smoke" sign)
**-**
Bupropion is **less likely** to cause **weight gain**
("stay fit lose weight" sign )
**-**Bupropion **doesn't** cause **sexual dysfunction**
("kissing couple below the basket")
88
what are the adverse effects of **Bupropion ?**
- can induce **Seizures**
* Bupropion is **contraindicated in Bulimia** since it can lead to seizures ("shaking popcorn binge snacker")
* Bupropion is **contraindicated in anorexia nervosa** since it can lead to seizures
("shaking skinny blacky player")
| ("shaking proball player dunking")
89
**Mirtazapine MOA**
| ("Mirth and Misery")
-Blocks **5HT-2/5HT-3 receptors**
("retired shirts number 52 and 53 hanging ")
--------------------------------------------------------------------------------
-Mirtazapine **blocks H1 receptors** leading to
* **weight gain** - good for depressed \*anorexic
* **sedation** - good for depressed with \*insomnia
--------------------------------------------------------------------------------
-blocks **α2 receptors** leading to **increased 5HT/NE**
("extinguished double candle above cam screen and released smiley/compass balloons")
90
**Trazodone MOA**
-Trazodone is a **Serotonin Modulator**
("marching drum player modulates serotonin smiley drum")
-**minimal effects** on NE/Dopamine therefore Trombone far from "NET DAT BALL"
--------------------------------------------------------------------------------
-**blocks 5HT-2** Receptors as well as **inhibits reuptake**
("marching drum player wearing retired shirt 52")
--------------------------------------------------------------------------------
-Trazodone is **α1 antagonist receptors**
("lady tromboner holding single extinguished candle ")
--------------------------------------------------------------------------------
-**inhibits H1** histamine receptors
("Bee swatter player")
91
Trazodone **adverse effects**
-Trazodone can cause **Priapism**
("TrazaBONER" male tromboner holding trombone in erected position)
-can cause **orthostatic hypotension {via α1 antag.}**
("coach fainting on floor")
-can cause **Sedation {via H1 antagonism}**
("sleeping players on bench")
-can cause **sexual dysfunction**
("trombone player rejected by female player because he is out of her league yo'")
-can cause **Serotonin Syndrome**
("pile of smiley balls on floor")
92
what can **Mirtazapine** b**e used for ?**
| ("Mirth and misery")
- Atypical Antidepressants _can be_ used as **1st line** treatment o**f depression** ("happy/sad mask" on cam screen):
* some patients with depression are adminstered with **Mirtazapine** as 1st line of treatment when the adverse effects are actually desirable e.g.- **elderly/anorexic** **{**usually SSRIs}
-Mirtazapine **doesn't** cause **sexual dysfunction**
("kiss-cam next to mirth/misery cam")
93
Name the **mood stabilizers**
| ("stabilizing ski poles")
**Lithium** ("lifthium lift")
**Valproate** ("winter festiVAL")
**Carbamazepine** ("classic car carved in ice")
**Lamotrigine** ("kid on dads head wearing Llama outfit")
**Antipsychotics** ("psychotic painting on high peak")
94
what is **lithium** useful for ?
| ("lifthium lift")
- lithium can treat **_bipolar disorder _**
* **acute mania** and **maintenance**
("stabilizing chair lift" on "lifthium lift")
95
what are the **side effects of lithium**
-has very **narrow therapeutic index**
("narrow window of opportunity to get off chair LIFTHIUM")
-lithium therapy can cause **hypothyroidism**
("pinguine on snowboard has undone bowtie") which presents with :
* **weight gain** ("fat ass snowboarder")
* dry skin
* hair loss
* constipation
-lithium can cause **nephrogenic diabetes insipidus** ("insipidus peeing kid fountain")
-diuretics like **thiazide** and **NSAIDs→** decrease **GFR** and **clearance** of lithium therefore **increase lithium** levels
("kid thighs on high dive" and pole saying "low clearance")
-lithium is **teratogenic** and can cause **Ebsitein's anomaly** ("tarantula hat on yellow shirt girl")
* **atrialization** of the **right ventricle** occurs as well as ASD and tricuspid valve defects
("large right snow head looks defected")
--------------------------------------------------------------------------------
**_acute lithium toxicity_**
* causes **GI symptoms [**nausea , vomiting ,diarrhea]
("early nauseated green shirt kid" )
**_chronic lithium toxicity_**
* neurologic symptoms-**tremor**
("late trembling blacky girl")
* neurologic symptoms-**ataxia**
("late falling black kid")
96
what **other drugs** can be used to treat **bipolar disorder?**
**Valproate** ("winter festiVAL" sign)
* acute mania and maintenance
**Carbamazepine** ("classic car carved in ice")
* acute mania and maintenance
**1st** [Haloperidol] and **2nd** [Quetiapine] **antipsychotics**
("psychotic paintings on high peak")
* acute mania
**Lamotrigine** ("child and dad wearing Llama outfit")
* maintenance only
97
name the **broad spectrum Antiepileptics**
("Seize the Land")
**Valproate**
("festiVAL reception)
**Topiramate**
("Toupee")
**Lamotrigine**
("Llama")
**Levetiracetam**
("Elevator")
98
broad spectrum antiepiletpics **MOA**
-Increase **Na+ channel **_in_**activation**
("inactivated baskets of salty peanuts")
-**metabolized** by the hepatic cytochrome **CYP450** system
("Chrome CYP450 canon on ship")
99
what are broad spectrum antiepileptic drugs **used for ?**
- **Focal** Seizures
- **Generalized** Seizures
- **Juvenile Myoclonic** Epilepsy (J.M.E)
100
**Valproate**
| ("welcome festiVAL")
-Increases **Na+ channel inactivation**
("inactivated baskes of salty peanuts")
-**increases GABA** levels in CNS
("elevated Cab of king of incas")
-can cause **GI distress** (nausea,vomiting)
("incas king is nauseated ")
-can cause **increased appetite** and **weight gain**
("king of incas is fat")
-can cause **Tremors**
("trembelling weapon baseball bat")
-can cause **Fatal hepatotoxicity**
("liver spot on inca cow")
-can cause **Pancreatitis**
("lady inca squeezing sponge")
-valproate can be **Teratogenic**
("Tarantula on inca shields")
-valproate therapy **during pregnancy** can cause **neural tube defects**
("inca has baby on her back playing the tubes")
101
**Topiramate**
| ("admiral's Toupee")
-increase **Na+ channel **_in_**activation**
("inactivated baskes of salty peanuts")
-**allosterically** binds to **GABA-A receptor**
("admiral shaking hand of Cab-A's inca driver")
-can cause **somnolence** and **fatigue**
("fatigued soldier behinnd admiral")
-can cause **confusion** and **cognitive slowing**
("soldier scratching his head behind admiral")
-can cause **weight loss**
("thin arm of canon operator")
-topiramate can cause **acute angle closure glaucoma**
("admirals helper holding high pressure eye kettle")
-topiramate may increase the risk for **Urolithiasis**
("canon balls next to admiral")
102
**Lamotrigine**
("Llama")
-increase **Na+ channels **_in_**activation**
("inactivated basket of salted peanuts")
-can cause **Stevens Johnson Syndrome** /Toxic epidermal Necrolysis {SJS/TEN}
("sloughed off mask of Llama rider")
-Llamotrigine may cause **diplopia**
("crossed eye camel")
103
**Levetiracetam**
("elevator")
-MOA not entirely known
-may cause **somnolence**
("sleeping elevator operator")
104
name the **narrow spectrum antiepileptics**
| ("Seize the night")
**Carbamazepine**
("classic car")
**Phenytoin**
("classic tow car")
**Gabapentin**
("Grab a pint! " on ice-cream parlor)
**Vigabatrin**
("raised V-Cab transmission")
**Tiagabine**
("tied up cab driver")
105
what can **narrow spectrum** antiepileptics be **used for ?**
- useful in treatment of **focal seizures**
- 2nd line agents used for maintainance during **status epilepticus**
106
**Carbamazepine**
("classic car")
-1st line therapy for **Trigeminal Neuralgia**
("three glowing gems")
--------------------------------------------------------------------------------
-increases **Na+ channel **_in_**activation**
("inactivated salty chip bags")
-induces **CYP450**
("classic car Activated chrome plate CYP450")
-can cause **ataxia**
("unbalanced stack")
-can cause **diplopia**
("misaligned headlights of classic car")
-can cause **D**rug **R**eaction with **E**osinophilia and **S**ystemic **S**ymptoms **S**yndrome {DRESS}
("eosinophilic dress of waiter 1")
-carbamazepine is **teratogenic**
("driver has tarantula shirt")
-may cause **Stevens Johnson Syndrome** (SJS) ("sloughed off mask of passenger next to driver of classic car ")
**--------------------------------------------------------------------------------**
-Carbamazepine can cause **SIADH**
("Inappropriate wet head of classic car driver")
-can cause **agranulocytosis**
("sand timer")
-carbamazepine therapy **during pregnancy** can cause **neural tube defects**
("neural tube exauhst")
107
**Phenytoin**
| ("classic tow car")
-increases **Na+ channel **_in_**activation**
("inactivated salty chip bags")
-induce**s CYP450**
("classic car Activated chrome plate CYP450")
-can cause **ataxia**
("unbalanced stack with waiter 2 ")
-can cause **diplopia**
("misaligned headlights of tow car")
-can cause **D**rug **R**eaction with **E**osinophilia and **S**ystemic **S**ymptoms syndrome {DRESS}
("eosinophilic dress of waiter 2")
-carbamazepine is **teratogenic**
("towed car driver has tarantula shirt")
-may cause **Stevens Johnson Syndrome (SJS)** ("sloughed off mask of towed car driver")
--------------------------------------------------------------------------------
-phenytoin may cause **folate deficiency** leading to **megaloblstic anemia**
("spilled salad above tow car")
-may cause **gingival hyperplasia**
("expanding gum")
-may cause **hirsutism**
("trucker with big bushy beard")
-phenytoin therapy **during pregnancy** may cause **cleft palate**
("trucker's cleft hat")
-can **decrease bone density**
("fractured osteoporotic towed car axle")
108
**Carbamazepine** and **Phenytoin** can both cause ...
("classic car and tow car")
drug-induced **Lupus**
| ("wolf between classic cars")
109
how should you treat **Status Epilepticus**
("order status" sign)
-treat acutely with **IV Benzodiazepines** Diazepam, Lorazepam and **Phenytoin** (2nd line) for maintenance
("Ben's diner in the background behind cars")
-if this treatment didn't work **IV Phenobarbital** can be used to treat **refractory seizures**
("barbershop in the background")
110
**Gabapentin**
| ("Grab a pint! " on ice-cream parlor)
-blocks **voltage gated Ca+2** channels
("closed Calci-YUM Ice cream cooler door")
-useful for treatment of **chronic pain**
("chronically frayed wire next to diasweeties machine")
-can treat **diabetic neuropathy**
("diasweeties machine ")
-useful for treatment of **Fibromyalgia**
("fiber bars in 1st row of diasweeties machine")
-useful in treatment of **post-herpetic neuralgia**
("Zeus poppin from top of ice cream car")
-can cause **ataxia**
("unbalanced stack of ice cream balls")
111
**Vigabatrin**
| ("raised V-Cab transmission")
**-irreversible** inhibition of **GABA-Transaminase** → **decrease** GABA degradation
("V-Cab _trans_mission")
112
**Tiagabine**
| ("tied up cab driver")
-inhibits GABA-**Reuptake**
("tied up driver can't be re-uptaken into cab")
113
**Absence Seizures** are characterized by ...
| ("Seize the day")
-type of **generalized seizure**
-sudden momentary **lapse in awareness** accompanied by **staring , blinking , clonic jerks**
("inattentive students")
-absence seizures manifest as **3 Hz spike wave** complexes on **EEG**
("3 spikes" sign on wall")
114
what are the **drugs** used for **treatment** of **Absence Seizures**
**Ethosuximide**
(modes of persuation:"ETHOS")
**Valproate**
("farm festiVAL")
**Lamotrigine**
("Llama outside the class")
115
**Ethosuximide**
| ("ETHOS")
-useful in treatment of **Absence seizures**
(teacher holding "absences" clip board)
**-Blocks** voltage gated **T-type Ca+2 channels** in the thalamus
(closed Calci-YUM chocolate milk drink next to T thermos")
-can cause **GI distress** ( nausea , vomiting)
("kid gets punched in stomach by bitch-ass bully")
-ethosuximide may cause **lethargy** and **fatigue**
116
**Valproate**
("farm fesiVAL")
-valproate is effective against **absence seizures**
117
**Lamotrigine**
| ("Llama" outside of class)
-Lamotrigine is effective against **absence seizures**
118
name the **high potency** 1st generation antipsychotics
("kid high on roof")
_"van gogh's starry g**AZIN**g" - **"azine"** suffix_
- **Haloperidol** ("halo of gazing star")
- **Trifluo**_per_**azine** ("kid **_try_**ing to **_fl_**y")
**-Flu**_phen_**azine (**"kid trying to **_fl_**y")
119
1st Generation antipsychotics **MOA**
-**block** dopamine **D2 receptors** in the CNS espeicalliy in **mesolimbic** and **striatofrontal** system
("Van Gogh holding double rope ")
-FGA's have **long half life** and thus long duration of action since they're **highly lipophilic**
("kid on crazy peak holding long tapered flag")
120
name the **low potency 1st Generation antipsychotics**
("van gogh's coloring tools on floor")
-**Thioridazine**
("color THEORYdazine")
**-Chloropromazine**
("color-pro" paint on floor)
121
what can **1st Generation** Antipsychotics be **used** for?
-can treat **_positive_** symptoms of **Schizophrenia-**hallucinations , delusions , disorganised thoughts
("Van Goch's right ear is cut off thus blocking positive voices")
-useful in treatment of **acute psychosis** in many condition {e.g. bipolar disorder}
("kid on crazy peak holding flag")
-may be used to treat **aggitation** , **aggression**
("kid on agitated peak with marionette")
-can be used for management of **Tourette syndrome**
("tourette's marionette with agitated aggressive blacky kid")
122
what are the **characteristic features** and **side effects** seen in **low potency** FGAs
**(low potency** \> high potency)
-they have **antimuscarininc effects** including
* dry mouth ("dry as a cracker")
* constipation
* blurred vision ("blind as a bat")
* urinary retention
-blocks **α1** receptors
("nurse holding single extinguished candle")
* leads to **orthostatic hypotension**
("passed out couple in picture")
**-**blocks **H1** histamine receptor
("nurse holding bee swatter")
* leads to **sedation**
("picture with Van Gogh's bed")
| ("alice in wonderland tea party picture")
123
what are the **characteristic features** and **side effects** seen in **High potency** FGAs
(low potency**\< high potency)**
-high potency FGAs cause **E**xtra **P**yramidal **S**ymptoms
* **Acute dystonia** ("Cocked head")/ in minutes
* **Akathisia** ("falling chair") /in days
* **Parkinsonism** ("cogwheels of carriage") /in weeks
-Can cause **Tardive dyskinesia**
("kid in carriage sticking out his tongue")
--------------------------------------------------------------------------------
-any drug blocking dopamine → **hyperprolactinemia** →galactorrhea, amenorrhea, impotence
("kfc kid has white mustache")
-------------------------------------------------------------------------------
-can cause **N**euroleptic **M**alignant **S**yndrome
(kfc bucket says "now more spicy")
* generalized **"lead pipe" rigidity**
* **altered mental** status, **fever**, autonomic **instability**
* characterized by **Rhabdomyolysis**
| ("kid on roof wearing extra pyramid hat")
124
* *Side effects** seen after adminstration of First Generation Antipsychotics
* *(low/high)**
-FGAs can cause **Torsades de Pointes** fatal cardiac arrhythmia ("twisted streamer")
-can **lower seizure threshold**
("shaking kid hanging on streamer")
125
**Chlorpromazine**
("color-pro paint")
-can cause **corneal deposits**
| ("corn yellow color-pro paint")
126
**Thioridazine**
| ("color THEORYdazine")
-can cause **retinal deposits**
("deposits on retinal color palette")
127
**name** the **2nd** generation (atypical) **antipsychotics**
| ("Dali the atypical surrealist")
**_"quite please only whispering is appropriate "_**
**Quetiapine**
("Quite")
**Olanzapine**
("Only")
**Risperidone**
("whispering")
**Aripiprazole**
("appropriate")
**Clozapine**
("**_clo_**zapine **_clo_**set")
**Ziprasidone**
("black dress zipper")
128
2nd generation (atypical) antipsychotics **MOA**
**-block** dopamine **D2** receptors in the CNS
("Dali holding double rope")
-**Block** serotonin **5HT-2A** receptor
("cut smiley cheese")
129
what can **2nd generation** (atypical) antipsychotics be **used for ?**
-SGAs are useful in treatment of both **positive** and **negative** symptoms of **Schizophrenia**
("Dali hearing both positive and negative voices")
**-**can treat **resistant depression**
("resisting bottle" from chateu tyramine)
**-**useful in managment of **OCD** adjunctive with SSRIs
("obssesively neat museum coworker aligning the pictures")
-can help manage **tourette syndrome**
( Dali holding "tourett's marionette")
130
what are the **side effects** associated with **2nd** generation (**atypical) antipsychotics**
_-block **H1** histamine receptors_
* causes **sedation**
("passed out brown piece of shit in painting")
_-blocks **α1** receptors_
("extinguished single candle on wall")
* causes **orthostatic hypotension**
("passed out brown piece of shit in painting")
-SGAs block muscarinic receptors and have **Antimuscarinic effects** especially Clozapine but in general **less** antimuscarinic effects **than FGAs**
* dry mouth
* constipation
* blurred vision
* urinary retention
("antimuscarinic tea party painting hanging _behind clozapine_ closet and _partialy covered_")
-SGAs , especially **Olanzapine** and **Clozapine** can cause
* **Weight gain**
("fat face of brown piece of shit in painting")
* ** Hyperglycemia**
("bunch of candy on floor of painting")
* **Dyslipidemia**
("elevated butter" in painting)
-SGAs can cause **torsade de pointes**
("twisted torsades streamer all over the damn place")
| (coworker with "bee swatter" hitting bee paintings)
135
**Clozapine**
("Clozapine Closet")
-can cause **Agranulocytosis**
("melting sand timers")
-can cause **myocarditis** and **cardiomyopathy**
("surreal heart in melting painting")
-clozapine **reduces seizures threshold**
("shaking clock in melting painting")
136
what is the **defining difference** between **1st** and **2nd generation** antipsychotics ?
- the **defining difference** is that in **2nd generation** drug therapy the **incidence** of **_E_**xtra **_P_**yramidal **_S_**ymptoms **is reduced [**EPS via blocking D2 Receptors]
("kid with EXTRA pyramid hat is causing disturbance and is asked to leave the exhibition")
_EPS include (FGA\>SGA)_
* acute dystonia
* akathisia
* Parkinsonism
\*\***Risperidone** has the **highest risk** of causing **EPS** among SGAs\*\*
("whispering kid whisperes to EXTRA pyramid hat kid")
-blocking **D2** receptors leads to **hyperprolactinemia** [FGA\>SGA]
("disturbing kid has milk mustache")
-------------------------------------------------------------------------------another difference is that the incidence of **_N_**euroleptic **_M_**alignant **_S_**yndrome is **also reduced** but is still possible [FGA\>SGA]
* NMS Includes mental status changes , rigidity , autonomic instability , fever
* NMS is associated with **rhabdomyolysis**
137
Name the Drugs used for **parkinson's disease**
**Levodopa**
_DOPA decarboxylase inhibitor_
**Carbidopa**
_COMT inhibitor_
**Entacapone
Tolcapone**
_MAOi B_
**Selegiline**
_D receptor agonists_
**Ropinirole
Pramipexole**
_Endogenous Dopamine enhancement_
**Amantadine**
_Antimuscarinic Drugs_
**Trihexyphenidyl
Benztropine**
139
side effects of Levodopa
-levodopa can cause **GI distress**
(due to peripheral conversion into dopamine)
- levodopa can cause **cardiac arrhythmias**
(due to peripheral conversion into dopamine)
-levodopa can cause **orthostatic hypotension**
(due to peripheral conversion into dopamine)
- levodopa can cause **neuropsychiatric symptoms** e.g. anxiety, agitation, insomnia, confusion, hallucination (due to excess dopamine in the CNS)
- chronic levodopa therapy can cause **response fluctuations** (wearing-off reaction, on-off phenomenon) and **dyskinesias**
-chronic levodopa therapy can cause a **wearing-off reaction**
(akinesia and dyskinesia re-emerge at the end of each dose)
-chronic levodopa therapy can cause an **on-off phenomenon**
(periods of akinesia alternate with periods of improved mobility, not related to dose)
-the **therapeutic window** of levodopa therapy **narrows** as Parkinson’s progresses
(unpredictable response to therapy) ("watch")
- chronic levodopa therapy can cause **dyskinesias** (choreoathetosis of the face and distal extremities)
- levodopa is **contraindicated** in **psychotic** patients
140
**Carbidopa**
- carbidopa (peripheral **DOPA decarboxylase inhibitor**)
- carbidopa **increases the bioavailability** of levodopa (prevents peripheral conversion into dopamine)
- carbidopa **decreases peripheral side** effects of levodopa therapy
(but exacerbates neuropsychiatric side effects)
141
Entacapone
Tolcapone
- (COMT) converts dopamine to (3-MT) in the CNS
- tolcapone (a _peripheral_ and central COMT inhibitor) increases the **bioavailability of levodopa**
- entacapone (a _peripheral_ COMT inhibitor) increases the **bioavailability of levodopa**
- tolcapone (a _peripheral_ and _central C_OMT inhibitor) increases dopamine levels in CNS
- tolcapone can cause **hepatic failure**
142
**Selegiline**
- monoamine oxidase B (MAO-B) selectively metabolizes dopamine
- selegiline -a selective MAO-B inhibitor **increases dopamine** levels in the **CNS**
143
**Ropinirole**
("rope in a role")
**Pramipexole**
("big pex")
**_Ropinirole_** (_D2_ dopamine receptor agonists)
is an **important initial treatment of Parkinson’s**
("Rope in a roll"):
**_Pramipexole_** (_D3_ dopamine receptor agonist)
is an **important initial treatment of Parkinson’s
----------------------------------------------------------------------------------**
- dopamine receptor agonists
(e. g. ropinirole, pramipexole) treat **restless leg syndrome** (RLS)
- --------------------------------------------------------------------------------
- dopamine receptor agonists (e.g. ropinirole) may **enhance impulse control disorders**
(e. g. gambling, shopping, hypersexuality)
144
**Amantadine**
- amantadine **enhances** the effect of **endogenous dopamine**
(by increasing its synthesis/release and inhibiting its uptake)
- amantadine can treat some **motor symptoms** of Parkinson’s
145
**Trihexyphenidyl
Benztropine**
-Trihexyphenidyl and Benztropine
(_antimuscarinic agents_ used to treat parkinsonism)
-trihexyphenidyl and benztropine (antimuscarinic agents) **improve tremor** and **rigidity** of Parkinson’s with no effect on bradykinesia
146
Levodopa metabolism
L-DOPA → Dopamine in periphery + CNS
Levodopa **can** cross BBB
Dopamine **can't** cross BBB
147
what is the **mechanism of action** by which opiates exert their effects ?
- opiates are **μ-opioid receptor agonists**
("μssage parlor")
-activation of opiate receptors leads to opening of **K+ ion channel** causing hyperpolarization
("open banana barrels in the back")
-activation of opiate receptors **closes Voltage Dependent Ca+2 channel**
("closed Calci-YUM ice cream cooler next to bananas")
-closure of Voltage Dependent Ca+2 channel **prevents release of neurotransmitters** basically stopping the pain signaling in the brain
("worker disconnecting presynaptic wire from icecream cooler")
149
Name the **Semi Synthetic opiates** and classify them according to their strength
**_Strong_**
Heroin
Oxycodone
**_Weak/Intermediate_**
Dihydrocodeine
**_Mixed Agonist/Antagonist_**
Buprenorphine
Nalbuphine
150
Tramadol **properties**
("synthetic weak/intermediate")
a **weak μ-opioid** receptor agonist used to manage chronic pain
* inhibits **reuptake of norepinephrine** and **serotonin**
("North-South")
| ("Distant tram")
151
Names of opiates agonists
**Fentanyl** (opioid analgesic)
("Fantasy”)
**Morphine** (opioid analgesic)
(“More fun")
**Tramadol**
("Distant tram")
(a weak μ-opioid receptor agonist used to manage chronic pain)
152
**Codeine**
("Barcode")
**Orphan**
("dextromethorphan")
**Properties**
**Opioid antitussives**
* dextromethorphan antagonizes **NMDA receptors**
("Tethered nomadic camel")
153
Opiates **Side Effects**
cause **CNS depression** (e.g.sedation)
("Cerebral towel")
-opiates can cause **respiratory depression**
("Deflated lung vest")
-opiates cause **miosis** (constricted pupils)
("Constricted hood")
-can cause **constipation**
("Plunger")
-can cause **biliary colic** (contract biliary smooth muscle)
("Biliary tree")
-patients may develop **tolerance** to opiates
(“All are welcome”)
* tolerance **does not develop for miosis** or **constipation**
("Out of order”")
-opiate induced **hyperalgesia** can occur with **chronic use**
("Causing pain")
-**opioid withdrawal**
("Anxious, hot, and moist")
* rhinorrhea
* lacrimation
* yawning
* hyperventilation
* hyperthermia
* muscle aches
* vomiting
* diarrhea
* anxiety
154
**Methadone**
("DONE timer")
**Properties**
**long acting** opioid used to **attenuate withdrawal** symptoms
* methadone and buprenorphine have a **long half lives** used in opioid detoxification
("Long tapering flag")
156
**Loperamide**
("Lop-eared rabbit")
**Diphenoxylate**
("Dolphins")
**properties**
**μ-opioid** receptors are located in the **GI tract** delay stool transit
* can be used as **antidiarrheals**
("Removed muddy slippers")
* Loperamid increases **colonic phasic segmentation →** increase stool transit time
("Loping back and forth")
160
**Buprenorphine**
Properties
long acting **partial μ-opioid** agonist used to **attenuate** **withdrawal** symptoms
161
_partial μ-opioid agonists_
**Buprenorphine
Nalbuphine
Butorphanol**
Properties
**partial μ-opioid** agonists can **induce withdrawals**
162
**Naloxone** use
("No lax zone")
**μ-opioid antagonist** used to **reverse acute** opioid **toxicity**
* can precipitate **withdrawals**
163
**Naltrexone** use
("No tricks zone")
**μ-opioid** antagonist
helps **maintain abstinence** in heroin addicts
("no tricks zone just results")
helps **reduce cravings** for **alcohol** and **nicotine**
("Tempting alcohol")
naltrexone can help with **weight loss**
("Getting fit")
164
Name the **Synthetic** Opiates
_Strong_
**Meperidine
Fentanyl
Methadone**
_Weak/ Intermediate_
**Diphenoxylate
Loperamide
Tramadol**
