This document discusses various opioid analgesics and their properties. It provides information on codeine, papaverine, noscapine, pholcodeine, dextromethorphan, pethidine, fentanyl, methadone, opioid use disorder, dextropropoxyphene, tramadol, pentazocine, nalbuphine, buprenorphine, butorphanol, nalorphine, naxolone, and naltrexone. It discusses their uses, mechanisms of action, adverse effects, and multiple choice questions related to these opioids.

1. OPIOIDS ANALGESICS

2. CODEINE
• CODEINE is Naturally Occurring Opium Alkaloid.
• It depresses the cough centre even in low doses.
• It is effective orally and well absorbed
• t is typically used to treat mild to moderate degrees of pain
• Greater benefit may occur when combined with paracetamol
(acetaminophen) or a nonsteroidal anti-inflammatory drug (NSAID)
such as aspirin or ibuprofen

3. • In Europe it is not recommended as a cough medicine in those
under twelve years of age.
• It typically starts working after half an hour with maximum effect
at two hours.
• The total duration of its effects last for about four to six hours.
• Codeine has less addiction liability and less chances of tolerance

4. ADVERSE EFFECTS
Common side effects include vomiting, constipation, itchiness, and
drowsiness.
Serious side effects may include breathing difficulties and
addiction. It is unclear if its use in pregnancy is safe.
Care should be used during breastfeeding as it may result in opiate
toxicity in the baby.
Its use as of 2016 is not recommended in children.

5. • CNS •
• little euphoria
• • minimal pain relief.
• • It may cause disorientation and
• excitement.

6. PAPAVERINE
• Papaverine (Latin papaver, "poppy") is an opium alkaloid
antispasmodic drug, used primarily in the treatment of visceral
spasm and vasospasm (especially those involving the intestines,
heart, or brain), and occasionally in the treatment of erectile
dysfunction.
• It is used in the treatment of acute mesenteric ischemia. While it
is found in the opium poppy, papaverine differs in both structure
and pharmacological action from the analgesic (morphine-related)
opium alkaloids (opiates).

7. NOSCAPINE
• NOSCAPINE is a naturally occurring opium alkaloid.
• In Therapeutic Doses, it has no other actions on the CNS except
for antitussive effects.

8. ADVERSE EFFECTS
• Nausea
• Vomiting
• Loss of coordination
• Hallucinations (auditory and visual)
• Swelling of prostate
• Loss of appetite
• Dilated pupils
• Increased heart rate
• Shaking and muscle spasms
• Chest pains
• Increased alertness
• Loss of any sleepiness

9. PHLOCODEINE
• Pholcodeine is a drug which is an opioid cough suppressant
(antitussive). It helps suppress unproductive coughs and also has a
mild sedative effect, but has little or no analgesic effects. It is
also known as morpholinylethylmorphine and homocodeine.
• Pholcodine is found in certain cough lozenges. However, in the UK,
the preparation is almost exclusively an oral solution, typically 5
mg / 5 ml. Adult dosage is 5-10 ml up to 3-4 times daily.

10. ADVERSE EFFECTS
• Side effects are rare and may include dizziness and
gastrointestinal disturbances such as nausea or vomiting.
• Adverse effects such as constipation, drowsiness, excitation,
ataxia and respiratory depression have been reported occasionally
or after large doses.

11. DEXTROMETHORPHAN
• Its structure is related to opioids.
• Its is an effective antitussive drug.
• It has no analgesic or addictive properties except antitussive
effect.

12. ADVERSE EFFECTS
• body rash/itching (see below)
• nausea
• vomiting
• drowsiness
• dizziness
• constipation
• diarrhea
• sedation
• confusion
• nervousness
• closed-eye hallucination
• A rare side effect is respiratory depression

13. PETHIDINE
• It is a derivative of morphine.
• Pethidine is 30 times more lipid soluble than morphine.
• • Oral bioavailability is 50%.
• • It is metabolized in the liver by ester hydrolysis to
• norpethidine and pethidinic acid that are excreted in the urine
• and therefore accumulate in renal failure.

14. • • Pethidinic acid is an inactive compound.
• • At higher concentration, norpethidine can produce
• hallucination and convulsions.
• • Pethidine is often used for labour analgesia. It readily crosses
• the placenta, and a significant amount reaches to the foetus
• over several hours.

15. PETHIDINE
• Pethidine is indicated for the treatment of moderate to severe
pain, and is delivered as a hydrochloride salt in tablets, as a
syrup, or by intramuscular, subcutaneous, or intravenous injection

16. ADVERSE EFFECTS [IN HIGHER DOSES] RARE CASE
• CNS
• Serious side effects like hypotension or
• hypertension, hyperpyrexia, convulsion and
• coma may occur.
• CVS
• Tachycardia, However as is the case with
• morphine, a significant decrease in BP may
• occur when pethidine is administered to elderly
• or hypovolaemic patients.

17. • GIS Dry mouth , It may produce less biliary tract
• spasm than morphine.
• EYE
• Meiosis is less
• Constipation and urinary retention are less common

18. FENTANYL
• Fentanyl (also spelled fentanil) is an opioid used as a pain
medication and together with other medications for anesthesia.
• Fentanyl is also made illegally and used as a recreational drug,
often mixed with heroin or cocaine. It has a rapid onset and
effects generally last less than an hour or two.
• Medically, fentanyl is used by injection, as a patch on the skin, as
a nasal spray, or in the mouth

19. ADVERSE EFFECTS
• Common side effects include vomiting, constipation, sedation,
confusion, hallucinations, and injuries related to poor
coordination.
• Serious side effects may include decreased breathing (respiratory
depression), serotonin syndrome, low blood pressure, addiction,
or coma.

20. METHADONE
• Its actions are similar to morphine
• It is effective analgesic
• It is effective by oral route
• It has long duration of action

21. USES
• Detoxification using methadone can either be done relatively
rapidly in less than a month or gradually over as long as six
months.
• While a single dose has a rapid effect, maximum effect can take
five days of use.The pain relieving effects last about six hours
after a single dose, similar to that of morphine.
• After long term use, in people with normal liver function, effects
last 8 to 36 hours. Methadone is usually taken by mouth and rarely
by injection into a muscle or vein.

22. OPIOID USE DISORDER
• Opioid use disorder is a problematic pattern of opioid use that causes significant
impairment or distress.
• Symptoms of the disorder include a strong desire to use opioids, increased
tolerance to opioids, failure to fulfill obligations, trouble reducing use, and
withdrawal syndrome with discontinuation.Opioid withdrawal symptoms may
include nausea, muscle aches, diarrhea, trouble sleeping, or a low mood.
• Addiction and dependence are components of a substance use
disorder.Complications may include opioid overdose, suicide, HIV/AIDS,
hepatitis C, marriage problems, or unemployment.
• Opioids include substances such as heroin, morphine, fentanyl, codeine,
oxycodone, and hydrocodone.

23. DEXTROPROPOXYPHENE
• It is a congener of methadone.
• It binds to the opioid receptors and produces effects similar ro
morphine.
• It is less constipating and is orally effective.
• It is an irritant when given parenterally.
• Large doses may cause CNS stimulation.
• It is used to control moderate pain.

24. ADVERSE EFFECTS
• Constipation
• Itching
• Drowsiness
• Sore throat
• Impaired alertness
• Confusion
• Serious or fatal heart rhythms
• Nausea

25. TRAMADOL
• Tramadol is phenylpiperidine
• analogue of codeine.
• It is weak agonist at all opioid receptors
• receptors.
• It inhibits neuronal
• reuptake of norepinephrine.
• It potentiates release of serotonin
• and causes descending inhibition
• of nociception

26. ADVERSE EFFECTS
• nausea, dizziness, dry mouth, indigestion, abdominal pain,
vertigo, vomiting, constipation, drowsiness and headache.
• Compared to other opioids, respiratory depression and
constipation are considered less of a problem with tramadol.

27. MIXED AGONISTS

28. PENTAZOCINE
• Pentazocine, sold under the brand name Talwin among others, is a
painkiller used to treat moderate to severe pain. It is believed to
work by activating (agonizing) κ-opioid receptors (KOR) and
blocking (antagonizing) μ-opioid receptors (MOR).
• As such it is called an opioid as it delivers its effects on pain by
interacting with the opioid receptors.
• Action is similar to the morphine.

29. AVERSE EFFECTS
• High dose may cause high blood pressure or high heart rate.
• It may also increase cardiac work after myocardial infarction when
given intravenously and hence this use should be avoided where
possible.
• Respiratory depression is a common side effect, but is subject to
a ceiling effect, such that at a certain dose the degree of
respiratory depression will no longer increase with dose increases.

30. NALBUPHINE
• is a opioid analgesic which is used in the treatment of pain.It is
given by injection into a vein, muscle, or fat.
• ADVERSE EFFECTS.
• sedation, sweatiness, clamminess, nausea, vomiting, dizziness,
vertigo, dry mouth, and headache.Unlike other opioids, it has
little to no capacity for euphoria or respiratory depression.
• It also has little to no incidence of dysphoria, dissociation,
hallucinations, and related side effects at typical therapeutic
doses

31. BUPRENORPHINE
• is an opioid used to treat opioid addiction, acute pain, and
chronic pain. It can be used under the tongue, by injection, as a
skin patch, or as an implant.
• It is highly lipid soluble synthetic opioid.
• It is 25times potent as morphine.
• Though onset of action is slow,duration of analgesia is long.
• CNS effects are similar to morphine while repiratory depression is
less.

32. ADVERSE EFFECTS
• Nausea and vomiting, drowsiness, dizziness, headache, memory
loss, cognitive and neural inhibition, perspiration, itchiness, dry
mouth, shrinking of the pupils of the eyes (miosis), orthostatic
hypotension, male ejaculatory difficulty, decreased libido, and
urinary retention and constipation.

33. BUTORPHANOL
• It is similar to pentazocine.

34. NALORPHINE
• It is a mixed opioid agonist–antagonist with opioid antagonist and
analgesic properties.
• At low doses,it is a good analgesic but it causes dysphoria amd
respiratory depression in low doses.
• At high, it acts as an antagonist and counters all the actions of
opioids.

35. • USES.
• Nalorphine may be used in acute opioid poisoning.
• It is also used for the diagnosis for the diagnosis of opioid
addiction.
• ADVERSE EFFECTS.
• restlessness, agitation, nausea, vomiting, a fast heart rate,
headache and sweating.

36. OPIOID ANTAGONISTS

37. NAXOLONE
• is a medication used to block the effects of opioids, especially in
overdose.
• Naloxone may be combined with an opioid (in the same pill) to
decrease the risk of misuse.
• When given intravenously, naloxone works within two minutes,
and when injected into a muscle, it works within five minutes,
• it may also be sprayed into the nose.

38. ADVERSE EFFECTS
• Sweating, nausea, restlessness, trembling, vomiting, headache.
• In rare cases been associated with heart rhythm changes and
seizures.

39. NALTREXONE
• It is a medication primarily used to manage alcohol or opioid
dependence.
• An opioid-dependent person should not receive naltrexone before
detoxification.
• It is taken by mouth or by injection into a muscle. Effects begin
within 30 minutes. A decreased desire for opioids, though, may
take a few weeks.
• Naltrexone is an opioid antagonist and works by blocking the
effects of opioids,

40. ADVERSE EFFECTS
• trouble
• Sleeping
• anxiety
• Nausea
• headaches.

41. MULTIPLE CHOICE QUESTIONS
• 1) __________ inhibits the reuptake of nor adrenaline and serotonin in CNS.
• A] Dextropropoxyhene B] Naloxone
• C] Tramadol D]Nalbuphine
• 2) Which form of fentanyl used for post operative obstetric analgesia.
• A] Epidural fentanyl B] Oral fentanyl
• C] Transdermal patches D] None

42. • 3) At the dose of 30 mg which drug has a ceiling effect.
• A] Dextropropoxyhene B] Nalophrine
• C] Both A & B D]Nalbuphine
• 4)Which of the following is naturally occurring opioid.
A] Noscapine B] Tramadol
C] Methadone D] Both B & C

43. • 5) Which of the following is K receptor agonist.
• A] Pentazocine B] Butorphanol
• C] Both A & B D] Methadone
• 6) Which drug is not suitable in Myocardial infarction.
• A) Fentanyl B) Pentazocine
• C) Naxolone D) All of the above

44. • 7) Which of the following is anti-tussive.
• A] Codeine B] Nascopine
• C] Phlocodeine D] All of the above
• 8) Fentanyl is given in combination with ________ to produce
neuroleptanalgesia.
• A] Droperidol B] Tramadol
• C] Butrophanol D] Both A & C

45. • 9) Morphine Addicts are given Methadone.
• A] Orally B] IV
• C] Inhalational D] IM
• 10) Which of the following is used for opioid blockade therapy in post addicts.
• A] Naxolone B] Naltexone
• C] Fentanyl D] Nalmefene
•

46. ANSWERS
• 1) TRAMADOL
• 2) EPIDURAL FENTANYL
• 3) NALBUPHINE
• 4) NASCOPINE
• 5) BOTH A & B
• 6) PENTAZOCINE
• 7) ALL OF THE ABOVE
• 8) DROPERIDOL
• 9) ORALLY
10) NALTEXONE