belladonna and opium

Action and Spectrum

When used together (e.g., in rectal suppositories for bladder spasms), belladonna’s anticholinergic action relaxes smooth muscle and reduces spasm, while opium provides analgesia and further reduces discomfort by blunting the pain pathways in the CNS. 

Drug Interaction

Adverse Reaction

Adverse drug reactions:   

>10%  

Nausea   

Urinary frequency   

Rhinitis  

Diaphoresis  

Headache   

Sweating  

Flushing   

Dizziness   

Chills   

1-10%  

Amblyopia  

Vomiting  

Hypertension   

Pain   

Asthenia  

Dyspepsia  

Lacrimation  

Frequency Not Defined  

Bradycardia  

Confusion  

Hypotension  

Tachycardia  

Increased airway resistance  

Black Box Warning

There is no blackbox warning 

Contraindication / Caution

Contraindication/Caution 

Contraindication 

 Hypersensitivity 

Cautions 

 Use carefully in patients with head injuries or high intracranial pressure. 

May worsen toxic psychosis or seizure disorders. 

Use caution in prostatic hyperplasia due to risk of urinary retention. 

Use carefully in heart disease, thyroid dysfunction, or myxedema. 

May cause biliary tract spasm; use caution in pancreatitis or biliary disorders. 

Risk of serious, even fatal, respiratory depression — monitor closely, especially when starting or increasing the dose; educate about signs of overdose. 

May cause severe low blood pressure or fainting; monitor in patients with cardiovascular disease, low blood volume, or shock. 

In patients with COPD, cor pulmonale, or reduced lung function, risk of dangerous respiratory depression — consider alternatives. 

Long-term use can affect hormones (adrenal insufficiency, hypogonadism) leading to bone loss or mood changes. 

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy Category: not assigned 

Breastfeeding warnings:  

The release of the drug into the human breastmilk is known 

Pregnancy Categories:      

Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.      

Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women      

Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans must take care of potential risks in pregnant women      

Category D: There is adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits      

Category X: Drugs listed in this category outweigh risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.      

Category N: There is no data available for the drug under this category  

Pharmacology

Belladonna and opium suppositories combine an anticholinergic agent with a narcotic analgesic to manage moderate to severe pain, particularly from ureteral spasms. Belladonna relaxes smooth muscle by blocking acetylcholine at muscarinic receptors, helping to reduce spasm. Opium provides pain relief by activating opioid receptors in the central nervous system, which blocks pain signals. Because opium is a narcotic, long-term use can lead to physical or psychological dependence. 

Pharmacodynamics 

Belladonna (mainly atropine and related alkaloids) works as an anticholinergic agent. It blocks muscarinic acetylcholine receptors in smooth muscle and glands, which reduces involuntary muscle spasms, decreases secretions, and relaxes the smooth muscle of the urinary tract. This helps to relieve painful ureteral spasms. Opium contains natural opioid alkaloids like morphine, which act as opioid receptor agonists, mainly at μ-opioid receptors in the brain and spinal cord. This activation inhibits pain signal transmission, providing significant analgesia and mild sedation. 

Pharmacokinetics 

Absorption
When administered rectally as a suppository, both belladonna alkaloids and opium alkaloids are absorbed through the rectal mucosa into systemic circulation. Opium’s analgesic effect typically starts within about 30 minutes, while belladonna’s antispasmodic effect may take 1–2 hours to reach peak action. 

Distribution
Both components distribute systemically. Opium alkaloids like morphine cross the blood-brain barrier to act on the central nervous system. Belladonna alkaloids (e.g., atropine) distribute to smooth muscle, secretory glands, and the CNS. 

Metabolism 

Opium: Primarily metabolized in the liver through conjugation with glucuronic acid to form active and inactive metabolites such as morphine-3-glucuronide and morphine-3,6-diglucuronide. 

Belladonna: Exact metabolic pathways are not well documented, but its alkaloids are expected to undergo hepatic metabolism similar to other tropane alkaloids. 

Elimination/Excretion 

Opium: Mainly excreted through the kidneys as glucuronide metabolites; a small amount is eliminated via bile. 

Belladonna: Primarily excreted in the urine. 

Adminstartion

Belladonna/opium suppositories are for rectal use only and should never be taken by mouth. The suppository should be inserted gently into the rectum, ideally after a bowel movement, following the exact dose and frequency prescribed by a healthcare provider. Patients should wash their hands before and after use, avoid exceeding the recommended dose or duration, and store the suppositories properly. Any suppository that appears damaged or discolored should be discarded. 

Patient Information Leaflet

Generic Name: Belladonna/opium 

Pronounced: bel-uh-DON-uh/ OH-pee-um 

Why do we use Belladonna/opium?  

Belladonna and opium suppositories are used to manage moderate to severe pain linked to ureteral spasms. This combination works as a narcotic pain reliever and antispasmodic to help relax smooth muscles and ease discomfort.