Opioids Flashcards by Yazan adnan

What type of receptors are all opioid receptors

G protein coupled that. Inhibit adenylyl cyclase Gi

reducing Ca2+ influx
reducing k+ efflux
reducing neuronal firing and transmitter release

How well did you know this?

Not at all

Perfectly

What doses are needed to control pain

High doses

How well did you know this?

Not at all

Perfectly

What are the symptoms of acute opioid toxicity

Respiratory depression 
Pinpoint pupils 
Coma 
Cyanosis
Apnea

How well did you know this?

Not at all

Perfectly

Opioid toxicity treatment

Ventilation and opioid antagonist -naloxone i.v

How well did you know this?

Not at all

Perfectly

What is morphine contraindicated in

In asthma and severe brain injury

How well did you know this?

Not at all

Perfectly

Adverse effects of morphine

MIOSIS (pinpoint eyes) - little tolerance - patho genomic for morphine in coma
out of it (sedation)
respiratory depression - tolerance develops
pneumonia (antitussive) - cough suppression
hypotension
infrequency (constipation and urinary retention)
nausea
emesis
causes release of histamine and euphoria. Analgesic.

How well did you know this?

Not at all

Perfectly

Most common cause of death with morphine

Respiratory depression

How well did you know this?

Not at all

Perfectly

Morphine therapeutic uses

Analgesic, treatment of diarrhea, relief of cough (antitussive), to treat acute pulmonary edema and anaesthesia.

How well did you know this?

Not at all

Perfectly

Effect of morphine on pregnant women

It can cross through the placenta and can cause addiction in infants and withdrawal symptoms

How well did you know this?

Not at all

Perfectly

Can morphine cross BBB

No it can’t

How well did you know this?

Not at all

Perfectly

Metabolites of morphine

M6G ( very potent analgesic)

M3G (Neurotoxic)

How well did you know this?

Not at all

Perfectly

Which side effects is it impossible to develop tolerance against

MIOSIS and Constipation

How well did you know this?

Not at all

Perfectly

What’s an opiate black box warning

Don’t give with benzodiazepines

How well did you know this?

Not at all

Perfectly

What’s a naturally occurring opiate

Codeine

How well did you know this?

Not at all

Perfectly

What is codeine used for

Used in mild to moderate pain

How well did you know this?

Not at all

Perfectly

What is codeine converted to and why

Morphine to show analgesic action

How well did you know this?

Not at all

Perfectly

What is codeine combined with for pain

Acetaminophen

How well did you know this?

Not at all

Perfectly

What’s a better alternative than codeine for antitussive effects and why

Dectromethorphan synthetic cough depressant with much lower abuse potential

How well did you know this?

Not at all

Perfectly

What is oxycodone

A semisynthetic analog

How well did you know this?

Not at all

Perfectly

What can oxycodone be used with

APAP, aspirin or ibuprofen - it can be used on its own too!

How well did you know this?

Not at all

Perfectly

When is hydromorphine preferred over morphine

In patients with renal dysfunction due to less active metabolite accumulation

How well did you know this?

Not at all

Perfectly

Hydrocodone uses and what can it be combined with

A good antitussive also combined with NSAIDs and APAP for pain

How well did you know this?

Not at all

Perfectly

What is Fentanyl related to

Chemically related to meperidine and is 100x more potent than morphine

How well did you know this?

Not at all

Perfectly

What is fentanyl used for

Used in anaesthesia and pain

- can be given as a transdermal patch used in reliefing cancer pain

How well did you know this?

Not at all

Perfectly

Fentanyl duration of action and uses

Rapid onset and short duration - Can be used with local anaesthetic - to provide analgesia for labour and post operative pain

When is fentanyl used as patches

For chronic pain (like cancer) with late offset and long duration

Meperidine structure in comparison with morphine

Is it structurally unrelated to morphine

Meperidine contraindications

Patients with impaired renal function

Meperidine special unique effect

AntiMuscarinic effect so have increased chance of delirium and mydriasis

What is meperidine metabolite

Normeperidine which is an active metabolite and is neurotoxic -> it is renally eliminated hence it is contraindicated in kidney failure

Meperidine clinical uses

Used in labour | Used in acute pain for a short time

Methadone receptors

Mu agonist as well as NMDA receptor antagonist

Effect of methadone on serotonin and norepinephrine

Uptake inhibitor

Methadone clinical uses

Used in the control of withdrawal effects of addicts and maintenance therapy because withdrawal symptoms with methadone are milder and prolonged

Methadone mode of elimination

Excreted in feces

Methadone adverse effects

It can cause QT prolongation and torsades des pointes

What are partial agonists and mixed agonist antagonist used for

Partial agonists given to opioid

What are partial agonists and mixed agonist antagonist used for

Partial agonists given to opioid naive can show agonistic response but when given to opioid addicts can show withdrawal symptoms

What are diphenoxylate and loperamide used for

Management of diarrhea

Petazocin receptors

Kappa agonist and weak atagonist or partial agonist of mu

Petazocin a mixed agonist and antagonist- effect

Can produce withdrawal symptoms in morphine abusers

Petazocin adverse effects

Increase in concentration can cause respiratory depression, tachycardia and hallucinations so it is rarely used

When is Petazocin used with caution

With angina and CAD

Buprenorphine receptors

Agonist at mu receptor and antagonist at Kappa receptor

Buprenorphine clinical uses

Used in the treatment of addiction—> used in opiate detoxification because it has a less severe and shorter duration of withdrawal than methadone

Buprenorphine mode of administration

Sublingual and subdermal formulation approved in treatment of opioid addiction due to providing prolonged suppression of opioid withdrawal

Why is Buprenorphine better than methadone at detoxification

Shorter and less severe

Buprenorphine adverse effects

Respiratory depression not easily reversed by naloxone also QT prolongation

Tramadol receptors

Centrally acting mu agonist which undergoes extensive metabolism to an active metabolite more affinity to mu receptors than parent compound

When is tramadol used

Used in moderate to severe pain

Tramadol adverse effects

Anaphylactoid reaction

Tapentadol receptors

Centrally acting analgesic and antagonist of mu receptors and NET inhibitor

Tapentadol clinical uses

Manage moderate to severe acute to chronic pain | Including neuropathic pain associated with diabetic peripheral neuropathy

Tapentadol should be avoided in which patients

Patients taking MAOIs within the last 2 weeks

Tapentadol metabolism

Metabolised by glucuronidstion —> low drug interactions

Tramadol drug drug interactions

SSRI MAOIs AND TCAs leading to CNS toxicity

Tramadol should be used with caution in people with

Seizures

Opioid antagonist

Naloxone and naltrexone

Naloxone mode of administration

Naloxone receptors

Competitive antagonist at mu kappa and deltts receptors | 10 time fold at mu> kappa

Naloxone clinical use

- Quick onset of action - Reverses respiratory depression and coma by opioid over dose 1-2 mins after IV administration - Could be used for withdrawal symptoms

Naltrexone difference than naloxone

Longer duration of action and slower onset of actions and can be given orally

Naltrexone mode of administration

Can be given as a sustained release IM/month

Naltrexone clinical use

Opioid dependence and alcohol addiction