Painkillers

Painkillers are analgesic medications. Pain is experienced when the special nerve endings in that part of the injured body send pain messages to the brain. Painkilling medicines interfere with these messages either at the site of the injury, in the spinal cord or in the brain and block the pain. Painkillers are available in different forms. They can be swallowed as tablets, capsules or liquids. There are painkillers in the form of injection, suppositories, creams or an ointment.

Painkiller abuse is on the rise all over the world and the US is possibly the largest consumer of Painkillers. One of the reasons is the easy availability of OTC Painkillers and possibly owing to the drug induced exuberance or 'high' associated with the intake of some kind of narcotic painkillers. The following pages offer a complete insight about the different types of Painkillers and their effects.

Painkiller categories

Pain killer medications are broadly classified into two main groups:

Non-narcotic (non-opioids)
Narcotic (opioid)

Common Non-narcotic painkillers: Non narcotic painkillers include two types, namely Non steroidal anti inflammatory drugs (NSAIDs) and Acetaminophen.

NSAIDs:

Aspirin - Actual drug name : Acetylsalicylic Acid is one of the widest known/used drugs to manage pain and to some extent fevers. With its anti-coagulant properties Aspirin is used for lowering the risk of heart attack and strokes in low doses.

Dosage: For Pain management in Adults: 3 gm per day in divided doses.
Lowering of the risk of heart attack and strokes (Myocardial Infarction - Prophylaxis or Thromboembolic Stroke Prophylaxis): - Single dose between 75 and 325 mg.

Ibuprofen : Another potent Analgesic in the NSAID group, Ibuprofen is useful to treat mild to moderate pain and helps to relieve symptoms of arthritis (osteoarthritis, rheumatoid arthritis or juvenile arthritis), such as inflammation, swelling, stiffness, and joint pain. It is also used as an Antipyretic and for symptomatic treatment of menstrual cramps.

Dosage: For Pain management in Adults: 200 - 400 mg every 4 hours in a day if administered orally. 400 - 800 mg if administered intravenously over a period of 30 minutes every 6 hours.

Naproxen : This NSAID is effective to control pain, stiffness and inflammation associated with conditions like arthritis, ankylosing spondylitis, Tendonitis, bursitis and gout.

Dosage: For Pain management in Adults: 500 mg Naproxen twice daily or in divided doses subject to a maximum of 1 gm per day.

Aceclofenac: Aceclofenac is a NSAID that is commonly used for its analgesic and anti-inflammatory properties. It is typically prescribed to treat various conditions such as rheumatoid arthritis, osteoarthritis, ankylosing spondylitis and other inflammatory disorders. Aceclofenac works by inhibiting the production of prostaglandins, which are substances responsible for pain, swelling, and inflammation. It primarily targets the enzyme cyclooxygenase (COX), specifically COX-2, thereby reducing pain and inflammation.

Dosage : The dosage of aceclofenac may vary depending on the patient's age, condition, and response. It is typically administered orally as tablets or capsules, with or without food. The recommended initial dose for adults is usually 100 mg twice daily.

Diclofenac : This NSAID is useful for pain management when there is inflammation such as Arthritis, Dermatomyositis and Ankylosing Spondylitis.

Dosage: For Pain management in Adults: 50mg tablets 3 times a day subject to a maximum of 150mg per day.

Indomethacin : This drug is prescribed for fever, pain, stiffness and swelling especially for relieving symptoms of swelling and pain related to osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. Indomethacin is effective also to treat acute shoulder pain and gouty arthritis.

Dosage: For Pain management in Adults: 25 - 50 mg every 8 hours subject to a maximum of 150 - 200 mg per day depending upon the severity of the pain.

Celecoxib: is used for rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, juvenile arthritis and menstrual pain.
Dosage:For Pain management in Adults: 200 mg once per day.

Narcotic painkillers:

• Codeine
  
• Fentanyl
  
• Meperidine
  
• Morphine
  
• Oxycodone
  
• Tramadol
  
• Hydrocodone
  
• Hydromorphone
  

NSAIDs provide relief from pain associated with inflammation. They are commonly used for headaches, fever, dental pain, dysmenorrhea, bone pain, arthritis and muscle aches. If prescribed alone, NSAID relieves slight to moderate pain and for moderate to severe pain relief, NSAIDs are used in combination with opioids. Some NSAID can be purchased over-the-counter and does not require a prescription from a medical doctor. Do not use this class of drug immediately before or after Coronary Artery Bypass Graft (CABG). Generally NSAIDs are not advisable when Dengue fever is present as this class of analgesics may induce capillary leakage which can lead to hemoconcentration and serous effusions resulting in circulatory collapse.

Acetaminophen: is available under many trade names. e.g.; Tylenol, Panadol
Paracetamol

Being an Analgesic and an Antipyretic (drug to reduce fever), Paracetamol (Acetaminophen) is used to treat many conditions such as headaches, muscles aches, arthritis, backache, toothaches, colds and fever caused by infection. Acetaminophen is available in the form of chewable tablets, capsules, liquid as well as in the form of suppositories. Acetaminophen can be taken after or before food unless specifically directed by the doctor.

Contraindication: Certain prescription medications when taken along with Paracetamol can cause problems. Paracetamol is not to be used without recommendation from a doctor under any of these circumstances.

• Liver problems
  
• Liver failure
  
• Excessive drinking of alcohol
  
• Allergy to Acetaminophen

Paracetamol during pregnancy

Paracetamol is not to be used by pregnant women without recommendation from the doctor. Taking Paracetamol while breast feeding can harm a nursing baby as Paracetamol can pass into breast milk. Signs of allergic reaction to Paracetamol include hives, difficulty breathing, and swelling of the face, lips, tongue or throat. Without further delay seek medical help.

Dosage: For Adults: 500 mg tablets every four hours per day subject to a maximum of 4 gms.

Narcotic painkillers: When the OTC painkillers do not provide the much needed relief from pain, narcotic painkillers are prescribed by the doctor. Narcotic are powerful painkillers effective in relieving severe pain. If not taken correctly or as directed by the doctor, narcotic painkillers can have serious side effects.

Codeine

Codeine is used to treat mild to moderately severe pain. It is also used to reduce severe cough and diarrhea. Codeine is available in the form of a tablet, a capsule, and a solution (liquid). Codeine can be taken with or without food. Narcotic medications should never be combined with alcohol as it can lead to dangerous side effects or even death. If there is a history of hypersensitivity to Codeine, it should not be prescribed. Also, Codeine is not to be used under these circumstance:

• Respiratory depression
  
• Acute or severe bronchial asthma or hypercarbia
  
• Symptoms of paralytic ileus. (bowel obstruction)
  
• Raised intracranial pressure

Codeine during pregnancy

FDA has categorized Codeine in Category C. Pregnant women or women planning to conceive should inform the doctor before using Codeine. If potential benefits outweigh potential risks, Codeine may be recommended for use during pregnancy. Codeine can pass into breast milk and may harm a nursing baby. Mild side effects include dizziness, lightheadedness, headache, drowsiness, mood change, nausea, vomiting, constipation, stomach pain and difficulty urinating. Serious side effects include difficulty in breathing, palpitations, hives, change in vision and seizures.

Fentanyl

Fentanyl is prescribed to treat pain in cancer patients. Fentanyl is particularly used for 'breakthrough pain', pain that is not controlled by other medicines. Fentanyl is usually not prescribed for treating or relieving pain other than cancer related. Fentanil is available in the form of buccal tablet, buccal film, nasal spray, oral transmucosal lozenge, transdermal film extended release. Fentanyl is not for casual use as this drug is far more potent than Morphine. Do not use this medication to relieve mild, short-term, or sudden pain.

Fentanyl is contraindicated for select health conditions and circumstances. Those with a known history of substance abuse should keep away from Fentanyl. If MAOI has been taken within 14 days, Fentanyl should be avoided as it may cause seizures, hyperthermia, and hypertension and in serious cases loss of life.

• Intolerance to any of the drug component.
  
• Hypotension
  
• Hypersensitivity
  
• Head injury
  
• Myasthenia Gravis
  
• Hypovolemia

Fentanyl during pregnancy

FDA has categorized Fentanyl in Category C. Pregnant women or women planning to conceive should inform the doctor before using Fentanyl. There is a possibility of addiction or withdrawal symptoms in newborns if the pregnant mother takes Fentanyl during pregnancy.

Meperidine

Meperidine (or Pethidine as it is commonly known)is prescribed to ease moderate to severe pain as determined by the doctor. In particular, Meperidine is used to ease pain that is experienced before or during surgery, for pain during labor and delivery. In some cases, Meperidine is prescribed for pain occurring from chronic conditions like sickle cell anemia and some type of cancers. Meperidine is available in the form of tablets as well as oral solution. Meperidine can be taken with or without food or as directed by doctor.

Pethidine is contraindicated in patients who are hypersensitive to Pethidine and those who have received recently. Also, patients who have breathing problems, respiratory depression, paralytic ileus, severe infectious diarrhea should avoid Meperidine. Do not take Meperidine while taking medicines like ritonavir, sibutramine or sodium oxybate.

Meperidine during pregnancy: FDA has categorized Meperidine in Category C. As there is a high possibility of respiratory depression in newborns, Meperidine should not be used in pregnant woman.

Side effects may be mild or severe. Less serious effects of Meperidine include constipation, loss of appetite, headache, feeling weak, dry mouth, excessive sweating, and unusual itching, below normal urinating, loss of interest in sex.

Morphine

Morphine is used for severe pain, cough suppression and sometimes before surgery. In most cases, Morphine is prescribed when the patient requires relief from pain for longer than a few days. Morphine is available in the form of capsules, oral solution, syrup or tablets. It is advantageous to drink plenty of liquid while taking Morphine.

Contraindication

Morphine is contraindicated in patients who have undergone surgery unless Morphine was used before surgery.

• Don't use Morphine in case of allergic reaction to narcotic medicines or narcotic cough medicines that contain codeine, hydrocodone or dihydrocodeine.
  
• If prone to asthma attack or a bowel obstruction, Morphine is not to be used.
  
• Dangerous drug interaction is possible if Morphine is used within 14 days of using a MAO inhibitor.
  
• Morphine is contraindicated in case of an undiagnosed abdominal pain, injuries of the head, chest injuries or depressed respiration and if the person is unconscious.

Morphine during pregnancy

FDA has categorized Morphine as Category C. Pregnant women or women planning to conceive should inform doctor before using Morphine. There is a possibility of addiction or withdrawal symptoms in newborn if the pregnant mother takes Morphine during pregnancy. Morphine can pass into breast milk and may harm a nursing baby.

Morphine side effects

There can be mild and severe side effects of Morphine. Look out for these side effects and remember to discuss with the doctor without delay. Besides these in case of any unusual body response, seek medical attention without delay.

• Shallow breathing
  
• Slow heart rate
  
• Seizures
  
• Cold clammy skin
  
• Severe weakness
  
• Trouble swallowing
  
• Pale skin
  
• Easy bruising
  
• Weight loss
  
• Constipation
  
• Memory problems
  
• Disturbed sleeping patterns.

Oxycodone

Similar to Morphine, Oxycodone is used for severe pain, cough suppression and sometimes before surgery. In most cases, Oxycodone is prescribed when the patient requires relief from pain for longer than a few days. Oxycodone is available in the form of a pill and liquid form. Drink plenty of water to avoid constipation. Oxycodone like many other Narcotic Pain Killers can be dangerous if alcohol is consumed. It is contraindicated for Asthma patients or those who suffer from paralytic ileus.

Oxycodone during pregnancy The FDA has assigned category B for Oxycodone. Unless the potential benefits outweigh the risks, Oxycodone is not given to pregnant women as this narcotic drug is habit forming. Though Oxycodone is excreted into breast milk, the potential effects are not well-established.

Tramadol

Tramadol is prescribed to relieve pain and is recommended for short term use only. Tramadol is effective in managing pain for rheumatoid arthritis, fibromyalgia and restless legs syndrome. Tramadol is available in the form of tablets, capsules, liquid and injection form.

Contraindication: Tramadol is contraindicated in patients who are suffering from epilepsy, previous head injury as it can induce seizures. Tramadol should not be prescribed to those with allergic reaction to any narcotic drug. Tramadol should not be taken with other medications like muscle relaxants, anti nausea medicines and anti depressants as it can exacerbate other underlying conditions.

Tramadol during pregnancy

The FDA has categorized Tramadol under category C. There are significant chances of the unborn baby developing problems and hence pregnant woman should not use Tramadol. Further, as Tramadol can pass into breast milk and harm a nursing baby, it should not be used while breast feeding.

Tramadol side effects

Most common side effects of Tramadol are constipation, diarrhea, drowsiness, dry mouth or nausea. If these persist seek medical attention immediately. Some of the serious side effects of Tramadol include severe or mild headaches, difficulty with swallowing, sudden mood swings, seizures, blurred vision, ringing in the ears and colored stools. Contact your doctor or go to the nearest emergency hospital.

Hydrocodone

Hydrocodone - a narcotic analgesic is usually available in combination with other ingredients like Paracetamol which contributes to better effect in pain control. There are Hydrocodone combinations to relieve moderate to severe pain and some to relieve cough. Hydrocodone is available in the form of tablet, capsule, syrup, solution and extended-release capsule as well as extended-release suspension. A normal diet would suffice unless specifically directed by doctor while using Hydrocodone.

Contraindication

Hydrocodone is contraindicated in patients with hypersensitivity to Hydrocodone or any ingredient of the formulation. Those with CNS (Central nervous system) depression and severe respiratory depression should avoid hydrocodone.

Hydrocodone during pregnancy

Hydrocodone is categorized under C by the FDA. As there is certain amount of risk associated, Hydrocodone is prescribed for pregnant women only if the potential benefits outweigh potential risks. Some of the side effects include nausea, headache, chest constriction, irregular heartbeat, allergic reactions and trouble urinating.

Hydromorphone

Hydromorphone is used to treat longer bouts of pain that do not respond to OTC painkillers. Being stronger than Morphine, hydromorphone is preferred to regulate pain from injuries, surgery, cancer and severe migraine headaches. Hydromorphone is normally given through parenteral administration as other ways of administrations result in poor absorption.

Contraindication

Hydromorphone is contraindicated in these circumstances.

• Allergy to hydromorphone or any other opioid medicines or any other ingredient of this medication.
  
• Has acute asthma or any other breathing problem.
  
• Has acute respiratory problem or severe central nervous system depression
  
• Has pulmonary edema.

Hydromorphone during pregnancy

As per FDA classification, Hydromorphone falls under category C. Unless, the potential benefits outweigh potential risks, doctors will not prescribe hydromorphone for pregnant women. Nausea and vomiting are very common side effects that occur initially. Serious side effects of Hydromorphone include allergic reaction, hives, confusion, severe weakness, losing consciousness and seizures. Seek medical attention immediately without any delay.

FDA Pregnancy Categories Drugs are divided into many categories based on the given drug and its effects on the fetus or its mother during pregnancy:

• Category A: Safe during Pregnancy based on studies on human
  
  
• Category B: Reasonably Safe - based on Animal studies
  
  
• Category C: Animal studies indicate possible risk - but the benefits may necessitate the use despite the risks
  
  
• Category D: Not Safe for fetus
  
  
• Category X: Do NOT use during Pregnancy as the potential for serious side effects is high
  
  

Hydromorphone

Also known as dihydromorphinone - it is a centrally acting narcotic pain medication used to relieve severe pain and severe coughing.

Side effects:
Can result in serious life threatening reactions for some individuals. Sedation, respiratory depression,dizziness, seizures, euphoria, low blood pressure, decreased heart rate, nausea, vomiting, sweating, constipation,urine retention and of course - addiction.

Precautions

Hydromorphone is faster acting compared with morphine and about 10 times stronger too. Patients with kidney problems must exercise caution when taking hydromorphone. It can potentiate the action of other drugs.

Normal dose:
Adults: oral, 2 mg every three to six hours as needed.

Cataplexy

Cataplexy is muscle weakness accompanied by typically triggered emotions such as laughing, crying or terror. These emotions are exhibited in full conscious awareness. The term cataplexy is derived from Greek 'Kata' meaning down, and 'plexis' meaning stroke. Cataplexy affects about 70% of those with narcolepsy. It is caused by autoimmune destruction of the neurotransmitter hypocretin which regulates arousal and wakefulness. Cataplexy without Narcolepsy (neurological disorder with symptoms of excessive daytime sleepiness, uncontrollable sleep and cataplexy) is rare and the cause is unknown.

Cataplexy Symptoms

Cataplexy manifests itself as muscular weakness. It can range from slackening of facial muscle to complete muscle paralysis with postural collapse. Severe attacks may result in inability to stand or move. Attacks are often brief and last from few seconds to about 30 minutes. This typically involves dropping the jaw, neck weakness and buckling of knees. The cataplectic attack is slow and progressive, so much so, the patient is usually able to avoid injury as they notice the feeling before the attack begins. As they are fully conscious during attacks, even extreme ones, they are aware of what is happening around them. Speech is slurred and vision may be impaired, it could be double vision or inability to focus, but hearing and awareness remain normal.

Cataplexy attacks

The hypothalamus region in the brain regulates basic functions of hormone release, emotions and sleep. During cataplexy, the neurochemical hypocretin is significantly reduced. Hypocretin is a primary chemical in regulating sleep as well as states of arousal and its deficiency can lead to decreased levels of histamine and epinephrine, chemicals that promote wakefulness, arousal and alertness.

Since cataplexy attacks are self-limiting, they resolve without the need for medical intervention. For instance, if the person is reclining comfortably, he/she may transition into sleepiness, hypnagogic hallucinations or a sleep onset period.

Cataplexy worsens with fatigue, and is different from narcoleptic sleep attacks. It is usually triggered by strong emotional reactions such as laughter, surprise, awe, embarrassment or by sudden physical effort, when a person is caught off guard. Such attacks could also occur spontaneously without any identifiable emotional trigger.

Cataplexy - Causes

Most have cataplexy with narcolepsy. Cataplexy is the most dramatic symptom of narcolepsy. And most cataplectic attacks are brought on by strong or extreme emotional feelings such as anger, stress, anxiety, depression and joy. Laughter and other positive emotions are the most common triggers of cataplexy. While the cause of cataplexy without narcolepsy is unknown, secondary cataplexy is linked to reduced levels of the chemical hypocretin, a neurotransmitter in the brain.

Secondary cataplexy is also associated with specific lesions located primarily in the lateral and posterior hypothalamus. Other conditions causing cataplexy include ischemic events, multiple sclerosis, head injury, Paraneoplastic syndromes and infections such as encephalitis. Cataplexy may occur transiently or permanently due to lesions of the hypothalamus caused by surgery especially in difficult tumor resections.

Recent ongoing research has found a clear association of Narcolepsy with an allele of the HLA gene family which provides instructions for the making a group of related proteins known as the Human Leukocyte Antigen (HLA) complex. This allele strongly increases the susceptibility for cataplexy. But 41% of patients without the explicit symptoms of cataplexy are carriers.

Diagnosis

Diagnosis of cataplexy is usually made by symptoms presentation. Excessive daytime sleepiness, sleep onset paralysis, hallucinations are some symptoms strongly evidencing cataplexy. A multiple sleep latency test is often conducted in order to quantify daytime sleepiness.

Treatment

There is no cure for cataplexy but is treated with medications to manage symptoms. There are no behavioral treatments. Those with narcolepsy often try to avoid thoughts and situations that they know are likely to evoke strong emotions as they know that these emotions are likely to trigger cataplectic attacks. Regardless of whether a person has narcolepsy or not, the doctor prescribes a selective serotonin and norepinephrine re uptake inhibitor to alleviate symptoms of cataplexy. Sodium oxybate is another effective drug for cataplexy.

However taking Xyrem and other sleep medications which are narcotic pain relievers or alcohol can lead to difficulty in breathing, coma and even can be fatal. In case of high blood pressure, diabetes, or other health problems, it is recommended to take medications only after consultations with the doctor.

Complications

Cataplexy is not a life threatening condition, unless engaging in potentially dangerous activities while experiencing an attack such as operating heavy machinery or driving motor vehicle. Sleep disturbances and sexual dysfunction can be caused by narcolepsy of which cataplexy is a primary symptom. As cataplexy is sudden, brief loss of voluntary muscle tone can be triggered by strong emotions such as laughter.

Cataplexy can occur during the waking hours and attacks can sometimes be rarely visible such as drooping of eyelids or severe total body collapse. As cataplexy is a neurological problem, chances are it can be misdiagnosed as a seizure disorder. As there is no cure for cataplexy, it has to be managed with medications and modifications of potential triggers.