summraize of pharma about opioid drug

1. Opioid
analgesics
Supervisor : dr. hussien
Anesthesia department

2. What is the ?
-Pain is defined as an unpleasant sensory
and emotional experience with actual or
potential tissue damage.
How we sense the pain ?
- specialized nerve endings called nociceptors
- harmful stimuli, such as extreme temperatures, pressure, or chemicals.
Activate these nociceptors  send signals spinal cord and brain 
sensation of pain is processed and interpreted.
Acute Pain
- Temporary
- results from an injury or illness
- as a warning signal
Chronic Pain
- longer period to healling
- result from conditions like arthritis or nerve
damage.

3. - Are chemical drugs that use to relief & reduce pain
- Derived from a plant called ( opium )
- Belong to family of drugs called ( opiate ) .
- This drugs are interact and binding with
(opioid receptors )inside the Human .
- OPIOID RECEPTOTS TYPE:
1- µ
2- Delta
3- KAPPA
- OVERVIEW OPIOID DRUGS:
1- morphine 2-mepridine 3- methadone 4-Fentanyl 5-Hydrocodone
6-Hydromorphone 7- oxycodone. 8- codeine 9- heroin
What are opioid

4. OPIOID RECEPTOTS TYPE / effect / location:

5. Classification of opoid drugs
- STRONG AGONIST
(MORPHINE , PETHEDINE , METHADONE , FENTANYL ,
ALFENTANYL , SUFENTANYL , REMIFENTANYL , OXYCODONE ,
OXYMORPHONE , HYDROMORPHONE)
-WEAK / LOW AGONIST
(codeine)
-MIXIED AGONIST AND ANTAGONIST DRUGS
(pentazocine & BUPRENORPHINE )
- OTHER ANALEGESICS
( TRAMADOL , TAPENTADOL )
- ANTAGONIST
( NALOXONE , NALTREOXNE)
Notes
Agonist opioids: These drugs activate opioid receptors
relieve pain by binding to and activating these receptors
Antagonist opioids: These drugs block or inhibit the activation of
opioid receptors. used to treat opioid overdose such as during
surgery. Naloxone is a commonly used opioid antagonist.
Mixed agonist-antagonist drugs have both agonistic and antagonistic
effects

6. 1-MORPHINE
- Strong agonist drug
- MECHANISM
Bind To Mu & KAPPA Receptors activation them
- ACTIONS
1- ANALGESIA
 relief pain with out loss of consciousness .
2-EUPHORIA
3- Respiratory depression
 make it less sensitivity to C02
4-Cough Reflex
 have anti-tussive codeine superior in this effect
5- Miosis
enhance parasympathetic stimulation result miosis
6- Emesis or Vomiting
stimulation of the chemoreceptor trigger zone (CTZ in the brain
that detects toxins and signals the vomiting center to induce
vomiting.
7- GIT  relief diarrhea . 8- CVS

7. therapeutic use
1- relief pain
2-Dirrhea : reduce GIT motility / increase anal sphincter
3- Cough : But codeine superior
4- pre-anesthetic medication
contraindications
1- HEAD INJURY
2- INFANT
3- LIVER & RENAL DISEASE
4- BRONCHIAL ASTHMA
5- ENDOCRINE DISEAESE

8. 2- meperidine
Introduction
- Strong agonist
- Synthetic opioid
- Use for treat acute pain
- Structurally unrelated to morphine .
MECHANISM OF ACTION
Bind to kappa and mu receptors
ACTIONS
- respiratory depression .
- Dilate pupil
- Less urinary retention
THERAPEUTIC USE
Analgesia , not use to treat diarrhea or cough ,
Use in obstetrics due its shorter duration & less depressant
On fetal
SIDE EFFECT
Pupillary dilation , hypotension , dry mouth , blurred vision
Convulsions , anxiety
3- Methadone
Introduction
- Strong agonist
- Synthetic opioid
- Use for treat acute pain
- analgesic activity similar to morphine but less euphoria .
MECHANISM OF ACTION
Bind to mu receptor
4- Fentanyl
Introduction
-Chemically synthetic related to meperidine
- Has 100 fold analgesic potency as morphine
- Highly lipid soluble & cross B.B.B
- Rapid onset & shorter duration action 15-30m
- Use for analgesia post operative & during labor
- Use in cardiac surgery because not act on myocardial contractility
- Unlike meperidine cause pupillary contraction .

9. MODRATE / LOE AGONIST
CODEINE( natural )
-
1- PENTAZOCINE
ACTION ON RECEPROES
- Its has agonist action kappa receptor and weak
antagonist action
on mu & delta receptors
USE
Produce analgesia by activation receptor on spinal cord to
relief pain
ADMINSTRATED & DURATION
Parentally or Orally , have short duration action
COMPARE WITH MORPHINE
Less euphoria
TOXCITY / SIDE EFFECT
1- in high dose cause respiratory depression & reduce Git
activity .
2- HIGH dose increase blood pressure cause hallucination
Tachycardia , dizziness .
3- Contraindication with patient suffer from angina cause
it
Increase work of heart .
4- Contraindication cause it decrease renal blood flow .
Introduction
- Less potent analgesic than morphine
- Highly effective orally
Action
- Good Anti – tussive at dose that not cause analgesia .
- Rarely dependence .
Compare with morphine
- Low potential for abuse than morphine
Combination
- Is often use in combination with Acetaminophen / asprin
MIX AGONIGST / ANTAGONIST
DRUG THAT STIMULATE ONE RECEPTOR AND BLOCK THE OTHER
CALLED ( MIXED AGONIST & ANTAGONIST )

10. -
2- BUPRENORPHINE
ACTION ON RECEPROES – it has partial agonist on mu
receptors & long duration of action
Adminstrated
It administered sublingually Or parenterally
USE
in opiate detoxification, because it has a less sever and
short duration of withdrawal symptoms compared to
methadone.
TOXCITY / SIDE EFFECT
It causes little sedation, resp. depression and hypotension
even at high doses.
MRTABLOISM / EXCRATION
It is metabolized in liver and excreted via bile and urine
TOXCITY & ADVERS EFFECT
Respiratory depression that cannot be reversed by
naloxone,nausea ,dizziness.
TRAMADOL (OTHER)
INTRO –
- It is centrally acting analgesic (synthetic)
- It binds to mu receptors
- also inhibits reuptake of norepinephrine and serotonin in
CNS .
Adminstrated
It is administered orally
USE
Treat moderate & sever pain
TOXCITY / SIDE EFFECT
respiratory depression less than morphine
MRTABLOISM / EXCRATION
It is metabolized in liver and excreted via bile and urine
TOXCITY & ADVERS EFFECT
Adverse effects: nausea, vomiting, dry mouth, dizziness,
sedation,it may cause anaphylaxis,seizures.
Contraindicated in patients with history of epilepsy.

11. -
ANTAGONSIT
- They rapidly reverse the effect of agonists. will normalize
respiration, level of consciousness, pupil size an bowel
activity.
- they have a rleatively high affinity for mu receptors but
they can also revese the agonists at delta and kappa
receptors.
1- Naloxone
WHAT IS ?
Opioid antagonism .
For what it use ?
Used to reverse the respiratory depression and coma due to Opioid over dose
- they have a relatively high affinity for mu receptors but they can also revese
the agonists at delta and kappa receptors.
MECHANISM
It rapidly displaces all receptor bound Opioid molecule and in this way reverse
the effects of opioid overdose. ONEST The effect is very fast,within 30
seconds of IV administration, the respiratory depression and coma characters
produced by over dose get reversed.
WHAT IS ?
Opioid antagonism .
For what it use ?
Single dose can block opioid effect for 48 hour
Duration ?
Have long duration action it proposed for maintenance for
For opioid addicts
Therapeutic use ?
it has been observed that naltrexone decrease craving for
alcohol in chronic alcoholics .
2- NalTREXONE

12. -
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