Pharmacology

Question 1

What blocks the effects of opioids?

Answer 1

Naloxone

Question 2

Describe opioid receptors

Answer 2

g-protein coupled receptors [Go/Gi]

Question 3

What are the main analgesic opioids?

Answer 3

μ [Mu] agonists

Question 4

Activation of opioid receptors produces …?

Answer 4

Inhibits adenylyl cyclase → Increases cGMP → pKA

Question 5

List opioids that are Mu agonists

Answer 5

Morphine
Codeine
Prthidine
Fentanyl

Question 6

List Mu antagonists

Answer 6

Naloxone

Naltrexone

Question 7

What drug of abuse is a mu agonist?

Answer 7

Heroin [diamorphine]

Question 8

What are the MOA of opioids?

Answer 8

Inhibits adenylyl cyclase → reduced cGMP → reduced pKA → no phosphyrlazation of channels

Activation of K conductance → hyper polarization

Inhibition of Ca conductance → reduced Ca entry into neurons → Reduced NT release and synaptic transmission

Question 9

Side effects of opioids?

Answer 9

Respiratory distress (→ death)
Constipation 
Pupilary contraction 
Bronchoconstriction 
Hypotension 
Pruritis

Question 10

Which opioid is used to treat diarrhea?

Answer 10

Loperamide

Question 11

What reverses tolerance to Opioids?

Answer 11

NMDA receptor antagonists

Ketamine
Dextromethorphan

Question 12

What treats opioids dependance?

Answer 12

Methadone

Question 13

Indications of weak opioids

Answer 13

Mild inflammatory arthritic pain, used in conjunctions with NSAIDs

Question 14

Indications of strong opoids

Answer 14

Severe acute pain
Cancer pain
Back pain
Severe arthritis

Question 15

Side effects of Morphine

Answer 15

Cough Suppression 
Constipation 
Euphoria
Analgesia 
Sedation 
Dependence 
Tolerance

Question 16

What form of morphine is the most potent?

Answer 16

M6G is more potent than morphine

Question 17

Indications of Codeine

Answer 17

Coughing

Question 18

MOA of Tramadol

Answer 18

Serotonin and NA re-uptake inhibitor [SNRI}

[partial Mu agonists]

Question 19

Contraindications of Tramadol

Answer 19

Suicidal patients

Question 20

What does Tramadol interact with?

Answer 20

Alcohol 
Narcotics 
Sedative
Anxiolytics
Anti-depressants

Question 21

What blocks the effects of Tramadol?

Answer 21

Naloxone [partially]

Question 22

Side effect of Pethidine

Answer 22

Bronchoconstriction

Question 23

Contraindications of Pethidine

Answer 23

Asthmatics

Question 24

What is the hard life of Fentanyl?

Answer 24

3-6 hrs. in the plasma

Question 25

Route of Administration of Fentanyl?

Answer 25

Sublingual | Transdermal

Question 26

Route of Administration of Codeine

Answer 26

Oral

Question 27

Route of Administration of Morphine

Answer 27

IV IM Orally Epidural route

Question 28

MOA of Methadone

Answer 28

NMDA receptor Antagonists

Question 29

What is used for treating addicts?

Answer 29

Methadone

Question 30

MOA of Naloxone

Answer 30

Mu antagonists

Question 31

What treats morphine dependence?

Answer 31

Morphine

Question 32

MOA of Naltrexone

Answer 32

Mu antagonists

Question 33

Duration of Naloxone and Naltrexone

Answer 33

naltrexone has a longer duration of action

Question 34

What role does GABA play in pain?

Answer 34

No role, rather it plays a role in epilepsy and anxiety

Question 35

What are orphan receptor?

Answer 35

receptors that don't have an affinity for opioid ligands

Question 36

Administration of morphine in RVM

Answer 36

Suppresses ON cells Activates Off cells Neutral cells

Question 37

What degrades 5HT in systole?

Answer 37

Monoamine Oxidase and Aldehyde Dehydrogenase

Question 38

What NT crosses BBB?

Answer 38

Tryptophan

Question 39

What is the role of Reserpine?

Answer 39

Transports of NA into vesicles

Question 40

What is the biochemical basis of depression?

Answer 40

Deficiency of monoamines [NA and 5HT]

Question 41

What is the biochemical basis of mania?

Answer 41

Overproduction of Monoamines [NA and 5HT]

Question 42

What effects do antidepressants produce in children >18 yrs?

Answer 42

Insomnia Aggression Worsening of Suicidal thoughts

Question 43

How can antidepressants induce seizures ?

Answer 43

Its lowers seizure threshold

Question 44

Onset of Antidepressants?

Answer 44

Beneficial effects within 2 weeks, maladaptive changes are produced earlier than beneficial

Question 45

MOA of imipramine

Answer 45

Inhibits neuronal re-uptake of NA and Serotonin into presynaptic nerve terminals Block 5HT, alpha Adrenergic, histamine and muscrainic receptors

Question 46

Indications of imipramine

Answer 46

Moderate-severe depression | Panic/Anxiety attacks

Question 47

Side effects of imipramine

Answer 47

``` Weight gain Orthostatic Hypotension Dizziness Reflex Tachycardia Arrhythmia Sudden death Blurred vision Dry mouth Urinary retention Constipation ```

Question 48

What drug interactions with imipramine produces toxic sedations?

Answer 48

Ethanol | CNS depressants

Question 49

What drug interactions with imipramine produces potentiation effects?

Answer 49

Direct acting adrenergic drugs

Question 50

What drug interaction with imipramine blocks its effect?

Answer 50

Indirect acting adrenergic drugs

Question 51

What precautions must be taken before prescribing imipramine?

Answer 51

Bipolar disorders [unmasks mania] | Suicidal patients [narrow TI]

Question 52

What drugs is a TCAs?

Answer 52

Imipramine

Question 53

What drugs are SSRIs?

Answer 53

Fluoxetine | Citalopram

Question 54

MOA of SSRIs

Answer 54

selectively inhibits serotonin re-uptake, and at higher doses can affect Na

Question 55

Indications of SSRIs

Answer 55

``` Moderate depression Bulimia nervosa OCD Anorexia Panic disorders ``` [dose reduced in hepatically impaired patients]

Question 56

Side effects of SSRIs

Answer 56

Anticholinergic ad cardiotoxic effects

Question 57

Half life of Fluoxetine

Answer 57

7-15 days

Question 58

Side effects of Fluoxetine

Answer 58

``` Nauseas Anxiety Insomnia Weight loss/Anorexia Tremors Sexual Dysfunction Seizures [overdose] ```

Question 59

MOA of Fluoxetine

Answer 59

Antagonist at 5HT2C and weak NA re-uptake inhibitor at higher doses

Question 60

MOA of SNRIs?

Answer 60

Inhibits reuptake of 5HT and NA

Question 61

What drugs are SNRIs?

Answer 61

Venlafaxine and Duloxetine