This document discusses opioids and their history, mechanisms, and modern uses. It begins by defining opioids as analgesics that bind to opioid receptors in the central nervous system and gastrointestinal tract. It then describes the classes of opioids including natural, semi-synthetic, and fully synthetic. The document outlines the long history of opioid use dating back thousands of years. It discusses morphine as the main active compound in opium and its role in medicine. The mechanisms of opioid receptors and their effects are explained. Potential side effects, addiction risks, and withdrawal symptoms are covered. Specific opioids like heroin, fentanyl, and their risks are examined. The document concludes by looking at modern opioid medications and future research.
Introduction.
Types of Diabetics Mellitus
Insulin and Insulin Preparations
Oral Hypoglycaemic Agents
Classification .
Drugs used in Anti-Diabetic agents
Mechanism of action .
Structure
Synthesis and SAR
Adverse Drug Reactions .
Uses.
Reference
This interesting ppt is the continuation of the Pharmacology of Opioid analgesics I... This impressive ppt highlight the pharmacology, advantages and disadvantages of opioid analgesics other than morphine with illustrations....!!
Introduction to Opioid analgesis, Terms, History, Classification, Morphine, Opioid receptors, Mechanism of action, Pharmacological actions of morphine, Pharmacokinetics, Adverse effects, Contraindications, Therapeutic uses
Presented by
B . Kranthi Kumar
Department of Pharmacology
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The term “opiate” refers only to substances with morphine-like activity that are structurally related to morphine. Opioids are sometimes referred to as “narcotic analgesics” and opioid receptor antagonists as “narcotic antagonists”
Introduction.
Types of Diabetics Mellitus
Insulin and Insulin Preparations
Oral Hypoglycaemic Agents
Classification .
Drugs used in Anti-Diabetic agents
Mechanism of action .
Structure
Synthesis and SAR
Adverse Drug Reactions .
Uses.
Reference
This interesting ppt is the continuation of the Pharmacology of Opioid analgesics I... This impressive ppt highlight the pharmacology, advantages and disadvantages of opioid analgesics other than morphine with illustrations....!!
Introduction to Opioid analgesis, Terms, History, Classification, Morphine, Opioid receptors, Mechanism of action, Pharmacological actions of morphine, Pharmacokinetics, Adverse effects, Contraindications, Therapeutic uses
Presented by
B . Kranthi Kumar
Department of Pharmacology
Myasthenia gravis (MG) is a chronic autoimmune disorder of the postsynaptic membrane at the neuromuscular junction (NMJ) in skeletal muscle. Circulating antibodies against the nicotinic acetylcholine receptor (achr) and associated proteins impair neuromuscular transmission
Concomitant use of Heparin and Telavancin or Oritavancin is contraindicated. Heparin may also interact majorly with other Anticoagulants such as Enoxaparin, Dalteparin, Bivalirudin, Danaparoid, Rivaroxaban, Apixaban and Dabigatran.
This presentation provides information about parkinsonism or Parkinson disease and pathophysiology, classification, pharmacological action and side effects of Anti Parkinson drugs.
The term “opiate” refers only to substances with morphine-like activity that are structurally related to morphine. Opioids are sometimes referred to as “narcotic analgesics” and opioid receptor antagonists as “narcotic antagonists”
Opioids and opiates are an important subject nowadays, especially because of the high level of lethal cases of overdose registered. There are multiple things that are good to know about these drugs and we tried to gather them all in this presentation.
Start a happier life leaving heroin or fentanyl abuse in the past, Call Renaissance Recovery Center, Gilbert, AZ
https://www.renaissancerecoverycenter.com/heroin-vs-fentanyl/
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Ethnobotany and Ethnopharmacology:
Ethnobotany in herbal drug evaluation,
Impact of Ethnobotany in traditional medicine,
New development in herbals,
Bio-prospecting tools for drug discovery,
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Opoid analgesics
1.
2. What are opioid analgesics?
History
Morphine
Mechanism of opioids
Side effects
Adverse reactions
Addiction, overdose and withdrawal symptoms
Opiophobia
Opioids of abuse
Heroin
Fentanyl
Future of opioids
3. Analgesics, or pain killers, that bind to opioid receptors which are
found principally in the:
CNS
Gastrointestinal tract
There are a number of broad classes of opioids:
Natural opiates
Alkaloids contained in the resin of the opium poppy including morphine,
codeine and thebaine
Semi-synthetic Opiates
Created from the natural opioids such as hydromorphone, oxycodone
and diacetylmorphine (heroin)
Fully synthetic opioids
Fentanyl, methadone and tramadol
Endogenous opioid peptides
Proudced naturally in the body, such as endorphins, enkephalins,
dynorphins and endomorphins
4.
5. Opioids have been the mainstay of pain treatment for thousand of
years, and they remain so today
The search for a safe, orally active, and non-addictive analgesic
based on the opiate structure is one of the oldest fields in medicinal
chemistry
The opiates are perhaps the oldest drugs known to humanity
The first undisputed reference to opium is found in the writings of
Theophrastus in the third century B.C.
The use of opium was recorded in China over 2000 years ago,
and was known in Mesopotamia before that
Its use in medicine is quoted in a twelfth-century prescription:
Take opium ,mandragora, and henbane in equal parts and mix
with water. When you want to saw or cut a man, dip a rag in this
and put it to his nostrils. He will sleep so deep that you may do
what you wish.
6. Opium contains a complex mixture of 20 alkaloids,
principle one being morphine
› Responsible for analgesic activity
Because of morphine’s poor oral bioavailability, it
was little used in medicine until the hypodermic
syringe was invented in 1853
Morphine was used during the American Civil War
and the Franco-Prussian war.
› Due to poor understanding about:
Safe dose levels
Effects of long-term use
And increased risks of addiction, tolerance and respiratory
depression
› Many casualties were either killed by overdoses or
became addicted to the drug
8. In general, opioids act
upon mu-, delta-, and
kappa-receptors on CNS
neurons producing:
Analgesia via
decreased
neuronal
transmitter
release and
decreased
nociceptive
impulse
propagation
Appears to work by
elevating the pain
threshold, thus
decreasing the brain’s
awareness of pain
Receptor
type
Location Effects
μ Brain,
spinal
cord
Analgesia, respiratory
depression, euphoria,
addiction, ALL pain
messages blocked
κ Brain,
spinal
cord
Analgesia, sedation, all
non-thermal pain
messages blocked
δ Brain Analgesia,
antidepression,
dependence
9. As with many drug therapeutics that cross the BBB and take
effect in the CNS, the mechanism of opioid derivatives is not
completely understood
For this reason, there is still biochemical/pharmacological
studies being conducted to try to understand how these drugs
work
A new study from last year was able to biotinylate various
opioid derivatives to aid in these types of studies which are still
very common
Biotinylation-process of covalently attaching a biotin (vitamin
H or B7) tag to a molecule or surface
10.
11. Dangerous side effects are those of
tolerance and dependence, allied with
the effects morphine can have on
breathing
› Most common cause of death from
morphine overdose is suffocation
› These side effects in one drug are
particularly dangerous and lead to severe
withdrawal symptoms when the drug is no
longer taken
15. A study was done in W. Virginia to evaluate persons dying
of unintentional pharmaceutical overdose, the types of
drugs involved and role of drug abuse in the deaths
Opioid analgesics were taken by 93.2% (275/295) of all
people who died of pharmaceutical overdoses in W.
Virginia in 2006
Only 44.4% (122/275) of those people had ever been
prescribed these drugs
The majority of overdose deaths in West Virginia in 2006
were associated with nonmedical use and diversion of
pharmaceuticals, primarily opioid analgesics
16. The fear of prescribing opioid
pain medications is known as
"opiophobia”
Goodman and Gillman’s
Pharmacological Basis of
Therapeutics insists that
although physical dependence
and tolerance may develop, this
should not in any way prevent
physicians from fulfilling their
primary obligation to ease the
patient’s discomfort
No patient should ever wish for
death because of a physician’s
reluctance to use adequate
amounts of effective opioids
Physical dependence is not
equivalent to addiction
17.
18. First synthesized in 1874
by an English chemist
but only became
popular more than 20
years later
From 1898 through
1910, under the name
heroin,
diacetylmorphine was
marketed as a non-
addictive morphine
substitute and cough
suppressant
19.
20.
21. A heroin overdose is usually treated with an opioid antagonist,
such as naloxone (Narcan) which has high affinity for opioid
receptors but does not activate them
Many fatalities reported as overdoses are probably caused by
interactions with other depressant drugs like alcohol or
benzodiazepines
It has been speculated that an unknown portion of heroin
related deaths are the result of an overdose or allergic reaction
to quinine, which may sometimes be used as a cutting agent
A final factor contributing to overdoses is place conditioning.
Heroin use is a highly ritualized behavior
23. 1959-Fentanyl first synthesized by Paul
Janssen under Janssen Pharmaceutica
1960s-Introduced as intravenous
anesthetic (Sublimaze)
1990’s-same company produced
Duragesic patch
Next came Actiq, flavored lollipop of
fentanyl citrate
Present-Effervescent tab for buccal
absorption and buccal spray device
24. The pharmaceutical industry has developed several analogues of
fentanyl:
Alfentanil (Alfenta), an ultra-short acting (5-10 minutes) analgesic
Sufentanil (trade name Sufenta), a potent analgesic (5 to 10 times
more potent than fentanyl) for use in heart surgery
Remifentanil (trade name Ultiva), currently the shortest acting
opioid, has the benefit of rapid offset, even after prolonged
infusions
Carfentanil (Wildnil) is an analogue of fentanyl with an analgesic
potency 10,000 times that of morphine and is used in veterinary
practice to immobilize certain large animals such as elephants
25. Fentanyl is normally sold on the black market in the form of
transdermal fentanyl patches such as Duragesic, diverted from
legitimate medical supplies
the patches may be cut up and eaten, or the gel from inside the
patch smoked
Another dosage form of fentanyl that has appeared on the streets is
fentanyl lollipops Actiq, which are sold under the street name of
"percopop”
They are sold for anywhere from $15-$40 per unit
Some heroin dealers mix fentanyl powder with larger amounts of
heroin in order to increase potency or compensate for low-quality
heroin, and to increase the volume of their product
As of December 2006, a mix of fentanyl and either cocaine or
heroin have caused an outbreak in overdose deaths in the United
States
The mixture of fentanyl and heroin is known as "magic" or "the
bomb", among other names, on the street
26.
27. Generic Name Brand Name
buprenorphine Buprenex
butorphanol Stadol
codeine Tylenol with codeine
fentanyl Duragesic
hydrocodone Vicodin
hydromorphone Dilaudid
methadone Dolophine
morphine Astramorph
oxycodone OxyContin
porpoxyphene Darvon
Opiods such as heroin and morphine exert their effects by mimicking naturally occurring substances, called endogenous opioid peptides or endorphins
Aromatic ring and N-methyl group also required, everything else can be modified
Nociceptive-causing pain. Mu-binds morphine strongest. K-safest analgesic due to less of the dangerous side effects
Discuss advantageous effects like eupohoria when treating terminally ill patients. Also, some provide clues to other possible uses of opiate-like structures. Widely used in cough medicines and treatment of diarrhoea
Change from –OH to –OAc facilitates heroin crossing BBB faster
Actually gets rapidly metabolized into morphine, pulled from market later
Other opioids of abuse do not form 6-MAM.
Other opioids being fentanyl, hydromorphone, oxycodone and pethidine/meperidine
80x more potent
Fentanyl is often used in cancer therapy and other chronic pain management due to its effectiveness in relieving pain. There is no known opioid stronger than Fentanyl in reducing cancer pain, which makes it the first choice for use in cancer patients.
Over 2008-09, a wide range of fentanyl preparations will become available, including buccal tablets or patches, nasal sprays, inhalers and active transdermal patches (heat or electrical).
To prevent accesibility of get to misuse, put drug in plastic matrix or inside silicone matrix. Sometimes heroin sold as fentanyl, which commonly lead to overdose
with the exception that many users report a noticeably less euphoric 'high' associated with the drug and stronger sedative and analgesic effects. Because the effects of fentanyl last for only a very short time, it is even more addictive than heroin, and regular users may become addicted very quickly. Additionally, fentanyl may be hundreds of times more potent than street heroin, and tends to produce significantly worse respiratory depression, making it somewhat more dangerous than heroin to users — though in some places, it is sold as heroin, often leading to overdoses.
Oral oxymorphone, 10X more potent. Oxidized –OH, additional hydroxyl group, and reduced double bond. 10% bioavailability, morphines is 15-30. ER and IR capsules
